Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T47768
(Former ID: TTDS00126)
|
|||||
Target Name |
Opioid receptor mu (MOP)
|
|||||
Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
Click to Show/Hide
|
|||||
Gene Name |
OPRM1
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 13 Target-related Diseases | + | ||||
1 | Acute pain [ICD-11: MG31] | |||||
2 | Bowel habit change [ICD-11: ME05] | |||||
3 | Chronic pain [ICD-11: MG30] | |||||
4 | Corneal disease [ICD-11: 9A76-9A78] | |||||
5 | Cough [ICD-11: MD12] | |||||
6 | Depression [ICD-11: 6A70-6A7Z] | |||||
7 | Digestive system disease [ICD-11: DE2Z] | |||||
8 | Irritable bowel syndrome [ICD-11: DD91] | |||||
9 | Large intestine motility disorder [ICD-11: DB32] | |||||
10 | Opioid use disorder [ICD-11: 6C43] | |||||
11 | Pain [ICD-11: MG30-MG3Z] | |||||
12 | Pruritus [ICD-11: EC90] | |||||
13 | Sensation disturbance [ICD-11: MB40] | |||||
Function |
Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B. Also couples to adenylate cyclase stimulatory G alpha proteins. The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4. Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization. Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction. The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins. The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation. Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling. Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling. Endogenous ligands induce rapid desensitization, endocytosis and recycling whereas morphine induces only low desensitization and endocytosis. Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties. Involved in neurogenesis. Isoform 12 couples to GNAS and is proposed to be involved in excitatory effects. Isoform 16 and isoform 17 do not bind agonists but may act through oligomerization with binding-competent OPRM1 isoforms and reduce their ligand binding activity. Receptor for endogenous opioids such as beta-endorphin and endomorphin.
Click to Show/Hide
|
|||||
BioChemical Class |
GPCR rhodopsin
|
|||||
UniProt ID | ||||||
Sequence |
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00768 ; BADD_A01328 ; BADD_A03957 ; BADD_A05200 ; BADD_A06356 | |||||
HIT2.0 ID | T66YJ0 |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 24 Approved Drugs | + | ||||
1 | Alfentanil | Drug Info | Approved | Anaesthesia | [2], [3] | |
2 | Alvimopan | Drug Info | Approved | Gastrointestinal disease | [4], [5], [6] | |
3 | Anileridine | Drug Info | Approved | Pain | [7], [8] | |
4 | Anileridine Hydrochloride | Drug Info | Approved | Pain | [9] | |
5 | Buprenorphine | Drug Info | Approved | Pain | [10], [11] | |
6 | Buprenorphine + naloxone | Drug Info | Approved | Opioid dependence | [9] | |
7 | Diphenoxylate | Drug Info | Approved | Diarrhea | [12], [13] | |
8 | Eluxadoline | Drug Info | Approved | Diarrhea-predominant irritable bowel syndrome | [14], [15] | |
9 | Fentanyl | Drug Info | Approved | Analgesia | [9] | |
10 | Hydrocodone | Drug Info | Approved | Pain | [16], [17] | |
11 | Hydromorphone | Drug Info | Approved | Pain | [9] | |
12 | Levomethadyl Acetate | Drug Info | Approved | Opioid dependence | [18], [19] | |
13 | Levopropoxyphene Napsylate Anhydrous | Drug Info | Approved | Cough | [9] | |
14 | Methadyl Acetate | Drug Info | Approved | Opioid dependence | [20] | |
15 | Methylnaltrexone bromide | Drug Info | Approved | Opioid-induced constipation | [5] | |
16 | Morphine | Drug Info | Approved | Chronic pain | [9] | |
17 | Naldemedine Tosylate | Drug Info | Approved | Opioid-induced constipation | [21], [22] | |
18 | Nalfurafine hcl | Drug Info | Approved | Uremic pruritus | [9] | |
19 | Naloxegol | Drug Info | Approved | Opioid-induced constipation | [9], [23], [24] | |
20 | Naloxone | Drug Info | Approved | Narcotic depression | [25], [26] | |
21 | Oxycodone | Drug Info | Approved | Pain | [27], [28] | |
22 | Propoxyphene Hydrochloride | Drug Info | Approved | Pain | [9] | |
23 | Remifentanil | Drug Info | Approved | Anaesthesia | [29], [30] | |
24 | Tapentadol hydrochloride | Drug Info | Approved | Acute pain | [5] | |
Clinical Trial Drug(s) | [+] 16 Clinical Trial Drugs | + | ||||
1 | GRT-6005 | Drug Info | Phase 3 | Diabetic neuropathy | [31] | |
2 | Morphine-6-glucuronide | Drug Info | Phase 3 | Pain | [32] | |
3 | NKTR-181 | Drug Info | Phase 3 | Neuropathic pain | [33] | |
4 | ALKS33 | Drug Info | Phase 2 | Alcohol dependence | [34] | |
5 | Met-enkephalin | Drug Info | Phase 2 | Pain | [35], [36] | |
6 | OPNT001 | Drug Info | Phase 2 | Eating disorder | [37] | |
7 | ORP-101 | Drug Info | Phase 2 | Irritable bowel syndrome | [38] | |
8 | TD-1211 | Drug Info | Phase 2 | Opioid-induced constipation | [39] | |
9 | TPM-1/Morphine | Drug Info | Phase 2 | Pain | [40] | |
10 | AIKO-150 | Drug Info | Phase 1 | Opioid dependence | [41] | |
11 | Cyt-1010 | Drug Info | Phase 1 | Pain | [42] | |
12 | GSK1521498 | Drug Info | Phase 1 | Obesity | [43] | |
13 | MCP-201 | Drug Info | Phase 1 | Pain | [44] | |
14 | NOCICEPTIN | Drug Info | Phase 1 | Headache | [45] | |
15 | SALVINORIN A | Drug Info | Phase 1 | Cerebral vasospasm | [46], [33] | |
16 | TRV734 | Drug Info | Phase 1 | Chronic pain | [33] | |
Discontinued Drug(s) | [+] 15 Discontinued Drugs | + | ||||
1 | ADL-5945 | Drug Info | Discontinued in Phase 2 | Constipation | [47] | |
2 | BCH-2687 | Drug Info | Discontinued in Phase 2 | Pain | [48] | |
3 | DPI-3290 | Drug Info | Discontinued in Phase 2 | Pain | [49] | |
4 | Frakefamide | Drug Info | Discontinued in Phase 2 | Pain | [48] | |
5 | MIRFENTANIL HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Pain | [50] | |
6 | Transdur-sufentanil | Drug Info | Discontinued in Phase 2 | Pain | [51] | |
7 | TREFENTANIL HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Pain | [52] | |
8 | ADL-7445 | Drug Info | Discontinued in Phase 1 | Constipation | [53] | |
9 | KN-203 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [54] | |
10 | VP004 | Drug Info | Discontinued in Phase 1 | Substance use disorder | [55] | |
11 | 443C81 | Drug Info | Terminated | Asthma | [57] | |
12 | BCH-150 | Drug Info | Terminated | Gastrointestinal disease | [58] | |
13 | DBO-11 | Drug Info | Terminated | Cancer related pain | [59] | |
14 | DBO-17 | Drug Info | Terminated | Cancer related pain | [60] | |
15 | Sameridine | Drug Info | Terminated | Pain | [61] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | GNTI | Drug Info | Preclinical | Obesity | [56] | |
2 | LY-25582 | Drug Info | Preclinical | Obesity | [56] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Agonist | [+] 38 Agonist drugs | + | ||||
1 | Alfentanil | Drug Info | [62] | |||
2 | Anileridine | Drug Info | [64] | |||
3 | Buprenorphine | Drug Info | [66], [67] | |||
4 | Buprenorphine + naloxone | Drug Info | [68] | |||
5 | Diphenoxylate | Drug Info | [69] | |||
6 | Levomethadyl Acetate | Drug Info | [76] | |||
7 | Methadyl Acetate | Drug Info | [77] | |||
8 | Remifentanil | Drug Info | [1] | |||
9 | Morphine-6-glucuronide | Drug Info | [84] | |||
10 | NKTR-181 | Drug Info | [85] | |||
11 | Carfentanil | Drug Info | [87] | |||
12 | Cyt-1010 | Drug Info | [93] | |||
13 | GSK1521498 | Drug Info | [43], [94] | |||
14 | MCP-201 | Drug Info | [95] | |||
15 | TRV734 | Drug Info | [33] | |||
16 | BCH-2687 | Drug Info | [99] | |||
17 | DPI-3290 | Drug Info | [100] | |||
18 | Frakefamide | Drug Info | [102] | |||
19 | MIRFENTANIL HYDROCHLORIDE | Drug Info | [9], [103] | |||
20 | Transdur-sufentanil | Drug Info | [104] | |||
21 | TREFENTANIL HYDROCHLORIDE | Drug Info | [9], [105] | |||
22 | KN-203 | Drug Info | [106] | |||
23 | DBO-11 | Drug Info | [84] | |||
24 | DBO-17 | Drug Info | [84] | |||
25 | 3-Methylfentanyl | Drug Info | [130] | |||
26 | 3-Methylthiofentanyl | Drug Info | [131] | |||
27 | Dihydromorphine | Drug Info | [163] | |||
28 | Dimethylthiambutene | Drug Info | [164] | |||
29 | DSLET | Drug Info | [82] | |||
30 | dynorphin B | Drug Info | [82] | |||
31 | ethylketocyclazocine | Drug Info | [82] | |||
32 | Ethylmorphine | Drug Info | [173] | |||
33 | Etorphine | Drug Info | [175] | |||
34 | NE-2 | Drug Info | [82] | |||
35 | normorphine | Drug Info | [82] | |||
36 | NRP290 | Drug Info | [82] | |||
37 | PL017 | Drug Info | [154] | |||
38 | TQ-1017 | Drug Info | [9] | |||
Antagonist | [+] 21 Antagonist drugs | + | ||||
1 | Alvimopan | Drug Info | [63] | |||
2 | Naldemedine Tosylate | Drug Info | [22] | |||
3 | Naloxone | Drug Info | [80], [81] | |||
4 | OPNT001 | Drug Info | [37] | |||
5 | AIKO-150 | Drug Info | [75], [92] | |||
6 | ADL-5945 | Drug Info | [98] | |||
7 | ADL-7445 | Drug Info | [98] | |||
8 | GNTI | Drug Info | [56] | |||
9 | LY-25582 | Drug Info | [56], [108] | |||
10 | ADC-5510 | Drug Info | [82] | |||
11 | AIKO-151 | Drug Info | [82] | |||
12 | Beta-endorphin | Drug Info | [146] | |||
13 | CTAP | Drug Info | [154] | |||
14 | CTOP | Drug Info | [144], [155] | |||
15 | Diprenorphine | Drug Info | [165] | |||
16 | KIN-4044 | Drug Info | [82] | |||
17 | KRP-100 | Drug Info | [82] | |||
18 | naloxonazine | Drug Info | [155] | |||
19 | naltriben | Drug Info | [82] | |||
20 | quadazocine | Drug Info | [82] | |||
21 | [3H]diprenorphine | Drug Info | [155] | |||
Modulator | [+] 24 Modulator drugs | + | ||||
1 | Anileridine Hydrochloride | Drug Info | [65] | |||
2 | Eluxadoline | Drug Info | [70] | |||
3 | Fentanyl | Drug Info | [71], [72] | |||
4 | Hydrocodone | Drug Info | [73], [74] | |||
5 | Levopropoxyphene Napsylate Anhydrous | Drug Info | [65] | |||
6 | Methylnaltrexone bromide | Drug Info | [5] | |||
7 | Morphine | Drug Info | [78] | |||
8 | Naloxegol | Drug Info | [9], [24] | |||
9 | Oxycodone | Drug Info | [82] | |||
10 | Propoxyphene Hydrochloride | Drug Info | [83] | |||
11 | Tapentadol hydrochloride | Drug Info | [5] | |||
12 | GRT-6005 | Drug Info | [31] | |||
13 | TD-1211 | Drug Info | [90] | |||
14 | 443C81 | Drug Info | [109] | |||
15 | BCH-150 | Drug Info | [110] | |||
16 | Sameridine | Drug Info | [112] | |||
17 | AIKO-152 | Drug Info | [82] | |||
18 | Endomorphins | Drug Info | [82] | |||
19 | KIN-3031 | Drug Info | [82] | |||
20 | KRP-110 | Drug Info | [82] | |||
21 | NCT-400 | Drug Info | [82] | |||
22 | NRT-300 | Drug Info | [82] | |||
23 | PTI-601 | Drug Info | [82] | |||
24 | Semorphone | Drug Info | [212] | |||
Inhibitor | [+] 427 Inhibitor drugs | + | ||||
1 | Hydromorphone | Drug Info | [75] | |||
2 | Nalfurafine hcl | Drug Info | [79] | |||
3 | ALKS33 | Drug Info | [86] | |||
4 | Met-enkephalin | Drug Info | [88] | |||
5 | ORP-101 | Drug Info | [89] | |||
6 | TPM-1/Morphine | Drug Info | [91] | |||
7 | NOCICEPTIN | Drug Info | [96] | |||
8 | SALVINORIN A | Drug Info | [97] | |||
9 | Dynorphin a | Drug Info | [101] | |||
10 | BIPHALIN | Drug Info | [111] | |||
11 | SB-213698 | Drug Info | [113] | |||
12 | SNF-9007 | Drug Info | [114] | |||
13 | (+/-)-nantenine | Drug Info | [115] | |||
14 | (+/-)-TRANS-U-50488 METHANESULFONATE | Drug Info | [116] | |||
15 | (-)-cyclorphan | Drug Info | [117] | |||
16 | (-)-eseroline | Drug Info | [116] | |||
17 | (H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) | Drug Info | [118] | |||
18 | 1,10-bis-(Dmt-Tic-amino)decane | Drug Info | [119] | |||
19 | 1,4-bis-(Dmt-Tic-amino)butane | Drug Info | [119] | |||
20 | 1,6-bis-(Dmt-Tic-amino)hexane | Drug Info | [119] | |||
21 | 1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane | Drug Info | [119] | |||
22 | 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [120] | |||
23 | 1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [120] | |||
24 | 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol | Drug Info | [120] | |||
25 | 1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol | Drug Info | [121] | |||
26 | 1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol | Drug Info | [121] | |||
27 | 1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol | Drug Info | [121] | |||
28 | 1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol | Drug Info | [121] | |||
29 | 1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol | Drug Info | [121] | |||
30 | 1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol | Drug Info | [121] | |||
31 | 1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol | Drug Info | [121] | |||
32 | 1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol | Drug Info | [121] | |||
33 | 1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol | Drug Info | [121] | |||
34 | 1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol | Drug Info | [121] | |||
35 | 1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol | Drug Info | [121] | |||
36 | 1-benzhydryl-4-(furan-2-yl)piperidin-4-ol | Drug Info | [121] | |||
37 | 1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol | Drug Info | [121] | |||
38 | 1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol | Drug Info | [121] | |||
39 | 1-benzhydryl-4-benzylpiperidin-4-ol | Drug Info | [121] | |||
40 | 1-benzhydryl-4-butylpiperidin-4-ol | Drug Info | [121] | |||
41 | 1-benzhydryl-4-cyclohexylpiperidin-4-ol | Drug Info | [121] | |||
42 | 1-benzhydryl-4-cyclopropylpiperidin-4-ol | Drug Info | [121] | |||
43 | 1-benzhydryl-4-ethoxy-4-phenylpiperidine | Drug Info | [120] | |||
44 | 1-benzhydryl-4-hexylpiperidin-4-ol | Drug Info | [121] | |||
45 | 1-benzhydryl-4-isopropylpiperidin-4-ol | Drug Info | [121] | |||
46 | 1-benzhydryl-4-m-tolylpiperidin-4-ol | Drug Info | [121] | |||
47 | 1-benzhydryl-4-methoxy-4-phenylpiperidine | Drug Info | [120] | |||
48 | 1-benzhydryl-4-o-tolylpiperidin-4-ol | Drug Info | [121] | |||
49 | 1-benzhydryl-4-p-tolylpiperidin-4-ol | Drug Info | [121] | |||
50 | 1-benzhydryl-4-phenyl-4-propoxypiperidine | Drug Info | [120] | |||
51 | 1-benzhydryl-4-phenylpiperidin-4-ol | Drug Info | [122] | |||
52 | 1-benzhydryl-4-tert-butylpiperidin-4-ol | Drug Info | [121] | |||
53 | 1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [123] | |||
54 | 1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [123] | |||
55 | 14-O-phenylpropylnaltrexone | Drug Info | [124] | |||
56 | 17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [125] | |||
57 | 17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [125] | |||
58 | 17-methyl-4'-methyldihydromorphinone | Drug Info | [126] | |||
59 | 17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate | Drug Info | [125] | |||
60 | 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide | Drug Info | [127] | |||
61 | 2-Benzylaminomethyl-3-hydroxymorphinan | Drug Info | [125] | |||
62 | 2-Hydroxymethyl-3-hydroxymorphinan | Drug Info | [125] | |||
63 | 3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone | Drug Info | [119] | |||
64 | 3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone | Drug Info | [119] | |||
65 | 3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone | Drug Info | [119] | |||
66 | 3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | Drug Info | [119] | |||
67 | 3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole | Drug Info | [128] | |||
68 | 3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol | Drug Info | [129] | |||
69 | 3-desoxy-3-carboxamidonaltrexone | Drug Info | [86] | |||
70 | 4-(4-((phenethylamino)methyl)phenoxy)benzamide | Drug Info | [132] | |||
71 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [133] | |||
72 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide | Drug Info | [134] | |||
73 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol | Drug Info | [135] | |||
74 | 4-phenyl-1-(1-phenylbutyl)piperidin-4-ol | Drug Info | [120] | |||
75 | 4-phenyl-1-(1-phenylethyl)piperidin-4-ol | Drug Info | [120] | |||
76 | 4-phenyl-1-(1-phenylheptyl)piperidin-4-ol | Drug Info | [120] | |||
77 | 4-phenyl-1-(1-phenylhexyl)piperidin-4-ol | Drug Info | [120] | |||
78 | 4-phenyl-1-(1-phenylpentyl)piperidin-4-ol | Drug Info | [120] | |||
79 | 4-phenyl-1-(1-phenylpropyl)piperidin-4-ol | Drug Info | [120] | |||
80 | 4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol | Drug Info | [120] | |||
81 | 4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol | Drug Info | [120] | |||
82 | 4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol | Drug Info | [120] | |||
83 | 5-(4-((phenethylamino)methyl)phenoxy)picolinamide | Drug Info | [132] | |||
84 | 6-(2-benzylisoindolin-5-yloxy)nicotinamide | Drug Info | [108] | |||
85 | 6-(2-phenethylisoindolin-5-yloxy)nicotinamide | Drug Info | [108] | |||
86 | 6-(4-((benzylamino)methyl)phenoxy)nicotinamide | Drug Info | [132] | |||
87 | 6-(4-((phenethylamino)methyl)phenoxy)nicotinamide | Drug Info | [108] | |||
88 | 6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide | Drug Info | [108] | |||
89 | 6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide | Drug Info | [132] | |||
90 | 6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide | Drug Info | [132] | |||
91 | 6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol | Drug Info | [136] | |||
92 | 6-desoxonaltrexone | Drug Info | [86] | |||
93 | 6beta-naltrexol HCl | Drug Info | [137] | |||
94 | 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide | Drug Info | [138] | |||
95 | 8-carboxamidocyclazocine | Drug Info | [139] | |||
96 | Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 | Drug Info | [140] | |||
97 | Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 | Drug Info | [140] | |||
98 | Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG | Drug Info | [141] | |||
99 | Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG | Drug Info | [141] | |||
100 | Ac-RYYRIK-K-(NH2)-YAFGYPS | Drug Info | [141] | |||
101 | Ac-RYYRIK-K-(NH2)-YRFB | Drug Info | [141] | |||
102 | Ac-YGGFL-NH2 | Drug Info | [142] | |||
103 | AKUAMMINE | Drug Info | [116] | |||
104 | AMINOFENTANYL | Drug Info | [143] | |||
105 | Antanal 1 | Drug Info | [144] | |||
106 | Antanal 2 | Drug Info | [144] | |||
107 | Benzyl derivative of M6G | Drug Info | [145] | |||
108 | Beta-funaltrexamine | Drug Info | [147] | |||
109 | Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate | Drug Info | [117] | |||
110 | BREMAZOCINE | Drug Info | [148] | |||
111 | BUTORPHAN | Drug Info | [149] | |||
112 | C6S | Drug Info | [150] | |||
113 | CARBOXYFENTANYL | Drug Info | [151] | |||
114 | Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [152] | |||
115 | Clocinnamox | Drug Info | [124] | |||
116 | CODEINONE | Drug Info | [153] | |||
117 | CYCLAZOCINE | Drug Info | [149] | |||
118 | CYCLORPHAN | Drug Info | [149] | |||
119 | CYPRODIME | Drug Info | [156] | |||
120 | C[L-Ala-D-pro-L-Phe-D-trp] | Drug Info | [140] | |||
121 | C[L-mTyr-D-pro-L-Phe-D-trp] | Drug Info | [140] | |||
122 | C[L-Phe-D-pro-L-mTyr-D-trp] | Drug Info | [140] | |||
123 | C[L-Phe-D-pro-L-Phe-D-trp] | Drug Info | [140] | |||
124 | C[L-Phe-D-pro-L-Phe-L-trp] | Drug Info | [140] | |||
125 | C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] | Drug Info | [140] | |||
126 | C[L-Phe-D-pro-L-Tyr-D-trp] | Drug Info | [140] | |||
127 | C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] | Drug Info | [140] | |||
128 | C[L-Tyr-D-pro-L-Phe-D-trp] | Drug Info | [140] | |||
129 | D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | [157] | |||
130 | D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) | Drug Info | [157] | |||
131 | D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) | Drug Info | [157] | |||
132 | D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | [157] | |||
133 | DADLE | Drug Info | [158] | |||
134 | DAMGO | Drug Info | [159] | |||
135 | DC6S | Drug Info | [150] | |||
136 | Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [160] | |||
137 | DELTORPHIN | Drug Info | [161] | |||
138 | DELTORPHIN-II | Drug Info | [162] | |||
139 | Deprotected cogener of M6G | Drug Info | [145] | |||
140 | DERMORPHIN | Drug Info | [141] | |||
141 | Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [160] | |||
142 | DIHYDROAKUAMMINE | Drug Info | [116] | |||
143 | Dimepheptanol | Drug Info | [136] | |||
144 | DM3A6S | Drug Info | [150] | |||
145 | DM3B6S | Drug Info | [150] | |||
146 | DM6S | Drug Info | [150] | |||
147 | Dmt-Pro-3,5Dmp-Phe-NH2 | Drug Info | [166] | |||
148 | Dmt-Pro-Dmp-Phe-NH2 | Drug Info | [166] | |||
149 | Dmt-Pro-Dmt-Phe-NH2 | Drug Info | [166] | |||
150 | Dmt-Pro-Emp-Phe-NH2 | Drug Info | [166] | |||
151 | Dmt-Pro-Imp-Phe-NH2 | Drug Info | [166] | |||
152 | Dmt-Pro-Mmp-Phe-NH2 | Drug Info | [166] | |||
153 | Dmt-Pro-Phe-D-1-Nal-NH2 | Drug Info | [167] | |||
154 | Dmt-Pro-Phe-D-2-Nal-NH2 | Drug Info | [167] | |||
155 | Dmt-Pro-Phe-Phe-NH2 | Drug Info | [166] | |||
156 | Dmt-Pro-Tmp-Phe-NH2 | Drug Info | [166] | |||
157 | Dmt-Pro-Trp-D-2-Nal-NH2 | Drug Info | [167] | |||
158 | Dmt-Sar-Phe-D-2-Nal-NH | Drug Info | [168] | |||
159 | DPDPE | Drug Info | [159] | |||
160 | Dynorphin(1-8) | Drug Info | [169] | |||
161 | ELAEOCARPENINE | Drug Info | [170] | |||
162 | ENDOMORPHIN 2 | Drug Info | [171] | |||
163 | ENDOMORPHIN-1 | Drug Info | [172] | |||
164 | ETONITAZENE | Drug Info | [174] | |||
165 | FALCARINDIOL | Drug Info | [176] | |||
166 | FLUPERAMIDE | Drug Info | [177] | |||
167 | H-2',6'-dimethyltyrosine-Tic-OH | Drug Info | [178] | |||
168 | H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH | Drug Info | [178] | |||
169 | H-Aba-ala-Gly-Phe-leu-OH | Drug Info | [88] | |||
170 | H-Aba-ala-Gly-Phe-Met-OH | Drug Info | [88] | |||
171 | H-Aba-Gly-Gly-Phe-Leu-OH | Drug Info | [88] | |||
172 | H-Aba-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [88] | |||
173 | H-Apa-ala-Gly-Phe-leu-OH | Drug Info | [88] | |||
174 | H-Cdp-ala-Gly-Phe-leu-OH | Drug Info | [88] | |||
175 | H-Cdp-Gly-Gly-Phe-Leu-OH | Drug Info | [88] | |||
176 | H-Cdp-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [88] | |||
177 | H-Cpa-Gly-Gly-Phe-Met-NH2 | Drug Info | [88] | |||
178 | H-Cpa-Gly-Gly-Phe-Met-OH | Drug Info | [88] | |||
179 | H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [179] | |||
180 | H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [179] | |||
181 | H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [179] | |||
182 | H-Dmt-Aba-Gly-NH-CH2-Bid | Drug Info | [180] | |||
183 | H-Dmt-Aba-Gly-NH-CH2-Ph | Drug Info | [180] | |||
184 | H-Dmt-Aba-Gly-NH-Ph | Drug Info | [180] | |||
185 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 | Drug Info | [181] | |||
186 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH | Drug Info | [181] | |||
187 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 | Drug Info | [182] | |||
188 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH | Drug Info | [182] | |||
189 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 | Drug Info | [182] | |||
190 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH | Drug Info | [182] | |||
191 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 | Drug Info | [182] | |||
192 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH | Drug Info | [182] | |||
193 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 | Drug Info | [182] | |||
194 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH | Drug Info | [182] | |||
195 | H-Dmt-Tic-Asp-N(Me)-Ph | Drug Info | [183] | |||
196 | H-Dmt-Tic-Asp-NH-Bzl | Drug Info | [183] | |||
197 | H-Dmt-Tic-Asp-NH-Ph | Drug Info | [183] | |||
198 | H-Dmt-Tic-D-Asp-N(Me)-Ph | Drug Info | [183] | |||
199 | H-Dmt-Tic-D-Asp-NH-Ph | Drug Info | [183] | |||
200 | H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) | Drug Info | [118] | |||
201 | H-Dmt-Tic-Glu-NH-(CH2)5-NH2 | Drug Info | [184] | |||
202 | H-Dmt-Tic-Glu-NH2 | Drug Info | [184] | |||
203 | H-Dmt-Tic-Gly-N(Me)-Ph | Drug Info | [183] | |||
204 | H-Dmt-Tic-Gly-NH-Bzl | Drug Info | [183] | |||
205 | H-Dmt-Tic-Gly-NH-CH2-Bid | Drug Info | [180] | |||
206 | H-Dmt-Tic-Gly-NH-Ph | Drug Info | [183] | |||
207 | H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph | Drug Info | [185] | |||
208 | H-Dmt-Tic-Lys(Ac)-NH-Ph | Drug Info | [185] | |||
209 | H-Dmt-Tic-Lys(Z)-NH-CH2-Ph | Drug Info | [185] | |||
210 | H-Dmt-Tic-Lys(Z)-NH-Ph | Drug Info | [185] | |||
211 | H-Dmt-Tic-Lys-NH-CH2-Ph | Drug Info | [185] | |||
212 | H-Dmt-Tic-Lys-NH-Ph | Drug Info | [185] | |||
213 | H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H | Drug Info | [186] | |||
214 | H-Dmt-Tic-NH-(CH2)6-NH-Phe-H | Drug Info | [186] | |||
215 | H-Dmt-Tic-NH-(CH2)6-NH-Tic-H | Drug Info | [186] | |||
216 | H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid | Drug Info | [185] | |||
217 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid | Drug Info | [183] | |||
218 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [183] | |||
219 | H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [183] | |||
220 | H-Dmt-Tic-NH-CH2-Boa | Drug Info | [187] | |||
221 | H-Dmt-Tic-NH-CH2-Bta | Drug Info | [187] | |||
222 | H-Dmt-Tic-NH-CH2-CH2-NH2 | Drug Info | [188] | |||
223 | H-Dmt-Tic-NH-CH2-Imid | Drug Info | [187] | |||
224 | H-Dmt-Tic-NH-CH2-ImidPh | Drug Info | [187] | |||
225 | H-Dmt-Tic-NH-CH2-Indl | Drug Info | [187] | |||
226 | H-Dmt-Tic-NH-CH2-Indn | Drug Info | [187] | |||
227 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid | Drug Info | [185] | |||
228 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid | Drug Info | [185] | |||
229 | H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid | Drug Info | [185] | |||
230 | H-mCpa-ala-Gly-Phe-leu-OH | Drug Info | [88] | |||
231 | H-mCpa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [88] | |||
232 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH | Drug Info | [152] | |||
233 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 | Drug Info | [189] | |||
234 | H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 | Drug Info | [189] | |||
235 | H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 | Drug Info | [189] | |||
236 | H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 | Drug Info | [189] | |||
237 | H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 | Drug Info | [190] | |||
238 | H-Tyr-c[D-Orn-Aic-Glu]-NH2 | Drug Info | [190] | |||
239 | H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 | Drug Info | [191] | |||
240 | H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 | Drug Info | [191] | |||
241 | H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Drug Info | [192] | |||
242 | H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac | Drug Info | [193] | |||
243 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H | Drug Info | [194] | |||
244 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [194] | |||
245 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [194] | |||
246 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc | Drug Info | [193] | |||
247 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [193] | |||
248 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [193] | |||
249 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [193] | |||
250 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | [194] | |||
251 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Drug Info | [192] | |||
252 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Drug Info | [192] | |||
253 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Drug Info | [192] | |||
254 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Drug Info | [192] | |||
255 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Drug Info | [192] | |||
256 | H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 | Drug Info | [191] | |||
257 | H-Tyr-Gly-Gly-Phe-Met-NH2 | Drug Info | [88] | |||
258 | H-Tyr-Pro-Ala-Phe-NH2 | Drug Info | [142] | |||
259 | H-Tyr-Pro-Dap(6DMN)-Phe-NH2 | Drug Info | [118] | |||
260 | H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 | Drug Info | [118] | |||
261 | H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H | Drug Info | [188] | |||
262 | H-Tyr-Tic-Cha-Phe-OH | Drug Info | [182] | |||
263 | H-Tyr-Tic-Phe-Phe-OH | Drug Info | [182] | |||
264 | HERKINORIN | Drug Info | [97] | |||
265 | HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 | Drug Info | [195] | |||
266 | ICI-199441 | Drug Info | [196] | |||
267 | KETOCYCLAZOCINE | Drug Info | [92] | |||
268 | KNT-5 | Drug Info | [197] | |||
269 | KNT-62 | Drug Info | [79] | |||
270 | KNT-63 | Drug Info | [79] | |||
271 | Leucine-enkephalin | Drug Info | [169] | |||
272 | LOFENTANIL | Drug Info | [198] | |||
273 | M3A6S | Drug Info | [150] | |||
274 | M3B6S | Drug Info | [150] | |||
275 | M3IBu6S | Drug Info | [150] | |||
276 | M3P6S | Drug Info | [150] | |||
277 | M3Pr6S | Drug Info | [150] | |||
278 | M3S | Drug Info | [150] | |||
279 | M6G thiosaccharide analogue | Drug Info | [145] | |||
280 | M6S | Drug Info | [150] | |||
281 | MC-CAM | Drug Info | [199] | |||
282 | MCL-117 | Drug Info | [117] | |||
283 | MCL-139 | Drug Info | [117] | |||
284 | MCL-144 | Drug Info | [200] | |||
285 | MCL-145 | Drug Info | [117] | |||
286 | MCL-147 | Drug Info | [201] | |||
287 | MCL-149 | Drug Info | [201] | |||
288 | MCL-153 | Drug Info | [202] | |||
289 | MCL-154 | Drug Info | [202] | |||
290 | MCL-182 | Drug Info | [201] | |||
291 | MCL-183 | Drug Info | [201] | |||
292 | MCL-428 | Drug Info | [203] | |||
293 | MCL-429 | Drug Info | [203] | |||
294 | MCL-431 | Drug Info | [203] | |||
295 | MCL-432 | Drug Info | [203] | |||
296 | MCL-433 | Drug Info | [203] | |||
297 | MCL-434 | Drug Info | [203] | |||
298 | MCL-435 | Drug Info | [203] | |||
299 | MCL-443 | Drug Info | [203] | |||
300 | MCL-444 | Drug Info | [203] | |||
301 | MCL-445 | Drug Info | [201] | |||
302 | MCL-446 | Drug Info | [201] | |||
303 | MCL-447 | Drug Info | [201] | |||
304 | MCL-448 | Drug Info | [201] | |||
305 | MCL-449 | Drug Info | [203] | |||
306 | MCL-450 | Drug Info | [204] | |||
307 | MCL-451 | Drug Info | [204] | |||
308 | MCL-457 | Drug Info | [201] | |||
309 | MCL-458 | Drug Info | [201] | |||
310 | METAZOCINE | Drug Info | [205] | |||
311 | MM3A6S | Drug Info | [150] | |||
312 | MM3B6S | Drug Info | [150] | |||
313 | MORPHICEPTIN | Drug Info | [171] | |||
314 | MORPHINONE | Drug Info | [153] | |||
315 | MR-1029 | Drug Info | [206] | |||
316 | MR-1526 | Drug Info | [206] | |||
317 | MR-2034 | Drug Info | [92] | |||
318 | MR-2266 | Drug Info | [206] | |||
319 | N-(17-Methylmorphinan-3-yl)-N'-phenylurea | Drug Info | [125] | |||
320 | N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea | Drug Info | [125] | |||
321 | N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 | Drug Info | [207] | |||
322 | N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 | Drug Info | [207] | |||
323 | N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 | Drug Info | [207] | |||
324 | N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine | Drug Info | [125] | |||
325 | N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine | Drug Info | [125] | |||
326 | N-isobutylnoroxymorphone | Drug Info | [208] | |||
327 | NalBzOH | Drug Info | [150] | |||
328 | Naltrexone-6-alpha-ol | Drug Info | [92] | |||
329 | NORBINALTORPHIMINE | Drug Info | [209] | |||
330 | O-DESMETHYL TRAMADOL | Drug Info | [92] | |||
331 | ORIPAVINE | Drug Info | [153] | |||
332 | OXYMORPHINDOLE | Drug Info | [174] | |||
333 | Oxymorphone semicarbazone hydrochloride | Drug Info | [169] | |||
334 | PHENAZOCINE | Drug Info | [92] | |||
335 | RTI-5989-31 | Drug Info | [210] | |||
336 | SB-0304 | Drug Info | [211] | |||
337 | SL-3111 | Drug Info | [213] | |||
338 | SN-11 | Drug Info | [113] | |||
339 | SN-23 | Drug Info | [113] | |||
340 | SN-28 | Drug Info | [214] | |||
341 | SOMATOSTATIN | Drug Info | [157] | |||
342 | SPIROINDANYLOXYMORPHONE | Drug Info | [215] | |||
343 | THEBAINE | Drug Info | [153] | |||
344 | Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [152] | |||
345 | Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 | Drug Info | [216] | |||
346 | Tyr-(R)-Aba-Gly-Phe-NH2 | Drug Info | [217] | |||
347 | Tyr-(R)-spiro-Aba-Gly-Phe-NH2 | Drug Info | [217] | |||
348 | Tyr-(S)-Aba-Gly-Phe-NH2 | Drug Info | [217] | |||
349 | Tyr-(S)-spiro-Aba-Gly-Phe-NH2 | Drug Info | [217] | |||
350 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
351 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
352 | Tyr-D-Ala-Gly-NMePhe | Drug Info | [147] | |||
353 | Tyr-D-Ala-Gly-Phe-Met-NH2 | Drug Info | [111] | |||
354 | Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Drug Info | [218] | |||
355 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [193] | |||
356 | Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
357 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
358 | Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 | Drug Info | [219] | |||
359 | Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 | Drug Info | [220] | |||
360 | Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 | Drug Info | [219] | |||
361 | Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 | Drug Info | [219] | |||
362 | Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 | Drug Info | [219] | |||
363 | Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 | Drug Info | [220] | |||
364 | Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
365 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
366 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
367 | Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
368 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
369 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
370 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [114] | |||
371 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
372 | Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
373 | Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [114] | |||
374 | Tyr-Pro-3,5Dmp-Phe-NH2 | Drug Info | [166] | |||
375 | Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 | Drug Info | [216] | |||
376 | Tyr-Pro-D-Phe-D-Pro-NH2 | Drug Info | [216] | |||
377 | Tyr-Pro-D-Phe-Pro-NH2 | Drug Info | [216] | |||
378 | Tyr-Pro-D-Phg-Phe-NH2 | Drug Info | [221] | |||
379 | Tyr-Pro-Dmp-Phe-NH2 | Drug Info | [166] | |||
380 | Tyr-Pro-Dmt-Phe-NH2 | Drug Info | [166] | |||
381 | Tyr-Pro-Emp-Phe-NH2 | Drug Info | [166] | |||
382 | Tyr-Pro-Hfe-Phe-NH2 | Drug Info | [221] | |||
383 | Tyr-Pro-Hfe-Pro-NH2 | Drug Info | [221] | |||
384 | Tyr-Pro-Imp-Phe-NH2 | Drug Info | [166] | |||
385 | Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 | Drug Info | [216] | |||
386 | Tyr-Pro-L-(NMe)Phe-Pro-NH2 | Drug Info | [216] | |||
387 | Tyr-Pro-L-Phe-D-Pro-NH2 | Drug Info | [216] | |||
388 | Tyr-Pro-L-Phe-Pro-NH2 | Drug Info | [216] | |||
389 | Tyr-Pro-Mmp-Phe-NH | Drug Info | [166] | |||
390 | Tyr-Pro-Phe-Ala-Bn | Drug Info | [222] | |||
391 | Tyr-Pro-Phe-D-2-Nal-NH2 | Drug Info | [168] | |||
392 | Tyr-Pro-Phe-D-Ala-Bn | Drug Info | [222] | |||
393 | Tyr-Pro-Phe-D-Phg-NH2 | Drug Info | [221] | |||
394 | Tyr-Pro-Phe-D-Val-Bn | Drug Info | [222] | |||
395 | Tyr-Pro-Phe-Hfe-NH2 | Drug Info | [221] | |||
396 | Tyr-Pro-Phe-Phe-N(CH3)2 | Drug Info | [223] | |||
397 | Tyr-Pro-Phe-Phe-NHCH3 | Drug Info | [223] | |||
398 | Tyr-Pro-Phe-Phe-NHNH2 | Drug Info | [223] | |||
399 | Tyr-Pro-Phe-Phe-OC(CH3)3 | Drug Info | [223] | |||
400 | Tyr-Pro-Phe-Phe-OCH2CH3 | Drug Info | [223] | |||
401 | Tyr-Pro-Phe-Phe-OCH2OH | Drug Info | [223] | |||
402 | Tyr-Pro-Phe-Phe-OCH3 | Drug Info | [223] | |||
403 | Tyr-Pro-Phe-Phg-NH2 | Drug Info | [221] | |||
404 | Tyr-Pro-Phg-Phe-NH2 | Drug Info | [221] | |||
405 | Tyr-Pro-Phg-Pro-NH2 | Drug Info | [221] | |||
406 | Tyr-Pro-Tmp-Phe-NH | Drug Info | [166] | |||
407 | Tyr-Pro-Trp-D-Ala-Bn | Drug Info | [222] | |||
408 | Tyr-Pro-Trp-D-Val-Bn | Drug Info | [222] | |||
409 | Tyr-Pro-Trp-Gly-Bn | Drug Info | [222] | |||
410 | Tyr-Sar-Phe-D-2-Nal-NH2 | Drug Info | [168] | |||
411 | UFP-502 | Drug Info | [162] | |||
412 | UFP-512 | Drug Info | [162] | |||
413 | YAWF-NH2 | Drug Info | [142] | |||
414 | YGGWL-NH2 | Drug Info | [142] | |||
415 | YGWFL-NH2 | Drug Info | [142] | |||
416 | YPAA-NH2 | Drug Info | [142] | |||
417 | YPWA-NH2 | Drug Info | [142] | |||
418 | YRFB | Drug Info | [141] | |||
419 | ZYKLOPHIN | Drug Info | [195] | |||
420 | [3H]U69593 | Drug Info | [150] | |||
421 | [D-Ala2]Met-enkephalinamide | Drug Info | [205] | |||
422 | [Dcp1]Dyn A(1-11)-NH2 | Drug Info | [160] | |||
423 | [Leu5]enkephalin | Drug Info | [224] | |||
424 | [Tyr-Pro-Phe-NH-CH2-]2 | Drug Info | [225] | |||
425 | [Tyr-Pro-Phe-NH-]2 | Drug Info | [225] | |||
426 | [Tyr-Pro-Phe-Phe-NH-CH2-]2 | Drug Info | [225] | |||
427 | [Tyr-Pro-Phe-Phe-NH-]2 | Drug Info | [225] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Drug Binding Sites of Target | Top | |||||
---|---|---|---|---|---|---|
Ligand Name: Morphine | Ligand Info | |||||
Structure Description | Morphine-bound mu-opioid receptor-Gi complex | PDB:8EF6 | ||||
Method | Electron microscopy | Resolution | 3.20 Å | Mutation | No | [226] |
PDB Sequence |
SMITAITIMA
75 LYSIVCVVGL85 FGNFLVMYVI95 VRYTKMKTAT105 NIYIFNLALA115 DALATSTLPF 125 QSVNYLMGTW135 PFGTILCKIV145 ISIDYYNMFT155 SIFTLCTMSV165 DRYIAVCHPV 175 KALDFRTPRN185 AKIINVCNWI195 LSSAIGLPVM205 FMATTKYRQG215 SIDCTLTFSH 225 PTWYWENLLK235 ICVFIFAFIM245 PVLIITVCYG255 LMILRLKSVR265 MLSGSKEKDR 275 NLRRITRMVL285 VVVAVFIVCW295 TPIHIYVIIK305 ALVTIPETTF315 QTVSWHFCIA 325 LGYTNSCLNP335 VLYAFLDENF345 KRCFREF
|
|||||
|
||||||
Ligand Name: Oliceridine | Ligand Info | |||||
Structure Description | Oliceridine-bound mu-opioid receptor-Gi complex | PDB:8EFB | ||||
Method | Electron microscopy | Resolution | 3.20 Å | Mutation | No | [226] |
PDB Sequence |
TAITIMALYS
78 IVCVVGLFGN88 FLVMYVIVRY98 TKMKTATNIY108 IFNLALADAL118 ATSTLPFQSV 128 NYLMGTWPFG138 TILCKIVISI148 DYYNMFTSIW158 TLCTMSVDRY168 IAVCHPVKAL 178 DFRTPRNAKI188 INVCNWILSS198 AIGLPVMFMA208 TTKYRQGSID218 CTLTFSHPTW 228 YWENLLKICV238 FIFAFIMPVL248 IITVCYGLMI258 LRLKSVRMLS268 GSKEKDRNLR 278 RITRMVLVVV288 AVFIVCWTPI298 HIYVIIKALV308 TIPETTFQTV318 SWHFCIALGY 328 TNSCLNPVLY338 AFLDENFKRC348 FREF
|
|||||
|
||||||
Click to View More Binding Site Information of This Target with Different Ligands |
Different Human System Profiles of Target | Top |
---|---|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Estrogen signaling pathway | hsa04915 | Affiliated Target |
|
Class: Organismal Systems => Endocrine system | Pathway Hierarchy |
Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 8.62E-05 |
---|---|---|---|---|---|
Closeness centrality | 2.05E-01 | Radiality | 1.36E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 2.07E+01 | Topological coefficient | 3.33E-01 | Eccentricity | 12 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | Estrogen signaling pathway | |||||
3 | Morphine addiction | |||||
NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
1 | TCR Signaling Pathway | |||||
Panther Pathway | [+] 3 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
3 | Enkephalin release | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | IL4-mediated signaling events | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Peptide ligand-binding receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | TCR Signaling Pathway | |||||
2 | GPCRs, Class A Rhodopsin-like | |||||
3 | Peptide GPCRs | |||||
4 | Opioid Signalling | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | The pro-nociceptive effects of remifentanil or surgical injury in mice are associated with a decrease in delta-opioid receptor mRNA levels: Prevent... Pain. 2009 Jan;141(1-2):88-96. | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7108). | |||||
REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075221. | |||||
REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7471). | |||||
REF 5 | 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6. | |||||
REF 6 | Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26. | |||||
REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7115). | |||||
REF 8 | Drug information of Anileridine, 2008. eduDrugs. | |||||
REF 9 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1670). | |||||
REF 11 | Buprenorphine for opioid dependence. J Pain Palliat Care Pharmacother. 2009;23(2):153-5. | |||||
REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7164). | |||||
REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040357. | |||||
REF 14 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7691). | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031329) | |||||
REF 16 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7081). | |||||
REF 17 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088017. | |||||
REF 18 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7212). | |||||
REF 19 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020315. | |||||
REF 20 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020315. | |||||
REF 21 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018 | |||||
REF 22 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
REF 23 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7539). | |||||
REF 24 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1668). | |||||
REF 26 | Opioid drug utilization and cost outcomes associated with the use of buprenorphine-naloxone in patients with a history of prescription opioid use. J Manag Care Pharm. 2008 Mar;14(2):186-94. | |||||
REF 27 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7093). | |||||
REF 28 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085910. | |||||
REF 29 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7292). | |||||
REF 30 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020630. | |||||
REF 31 | Cebranopadol: a first in-class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist. Br J Anaesth. 2015 Mar;114(3):364-6. | |||||
REF 32 | ClinicalTrials.gov (NCT01082471) An Efficacy and Safety Study to Compare Morphine 6-glucuronide (M6G) and Morphine in Patients Suffering With Post-Operative Pain for at Least 24 Hours. U.S. National Institutes of Health. | |||||
REF 33 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 34 | Clinical pipeline report, company report or official report of Alkermes. | |||||
REF 35 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1614). | |||||
REF 36 | ClinicalTrials.gov (NCT00109941) Opioid Growth Factor in Treating Patients With Advanced Pancreatic Cancer That Cannot Be Removed By Surgery. U.S. National Institutes of Health. | |||||
REF 37 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 38 | ClinicalTrials.gov (NCT04129619) A Double-Blind, Placebo-Controlled, Phase 2, Responsive Adaptive Randomization Study of ORP-101 in Patients With Irritable Bowel Syndrome With Diarrhea (IBS-D). U.S.National Institutes of Health. | |||||
REF 39 | ClinicalTrials.gov (NCT01401985) A Study of TD-1211 in Subjects With Opioid-Induced Constipation (OIC). U.S. National Institutes of Health. | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023017) | |||||
REF 41 | ClinicalTrials.gov (NCT00829777) Safety Study of Intravenous 6 Naltrexol (AIKO-150) in Opioid-Dependent Subjects. U.S. National Institutes of Health. | |||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035166) | |||||
REF 43 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2011). | |||||
REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018011) | |||||
REF 45 | ClinicalTrials.gov (NCT01404091) A Study of Nociceptin/Orphanin FQ Peptide Receptor Occupancy in Healthy Subjects. U.S. National Institutes of Health. | |||||
REF 46 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030930) | |||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009073) | |||||
REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010668) | |||||
REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003921) | |||||
REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015205) | |||||
REF 52 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003192) | |||||
REF 53 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031260) | |||||
REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026307) | |||||
REF 55 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025668) | |||||
REF 56 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
REF 57 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000227) | |||||
REF 58 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003724) | |||||
REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009577) | |||||
REF 60 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009580) | |||||
REF 61 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005282) | |||||
REF 62 | Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87. | |||||
REF 63 | Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77. | |||||
REF 64 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. | |||||
REF 65 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 66 | Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8. | |||||
REF 67 | Partial versus full agonists for opioid-mediated analgesia--focus on fentanyl and buprenorphine. Acta Anaesthesiol Belg. 2002;53(3):193-201. | |||||
REF 68 | Abstracts of Poster Presentations: CNS Summit 2013: November 14-17, 2013 Boca Raton, Florida. Innov Clin Neurosci. 2013 Nov-Dec; 10(11-12 Suppl B): 1-18. | |||||
REF 69 | Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. | |||||
REF 70 | Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56. | |||||
REF 71 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
REF 72 | Synthesis and pharmacological studies of new hybrid derivatives of fentanyl active at the mu-opioid receptor and I2-imidazoline binding sites.Bioorg Med Chem.2006 Oct 1;14(19):6570-80. | |||||
REF 73 | Clinical pipeline report, company report or official report of kempharm. | |||||
REF 74 | The Relative Abuse Liability of Oral Oxycodone, Hydrocodone and Hydromorphone Assessed in Prescription Opioid Abusers | |||||
REF 75 | Clinical pipeline report, company report or official report of signaturerx. | |||||
REF 76 | Methadone-related opioid agonist pharmacotherapy for heroin addiction. History, recent molecular and neurochemical research and future in mainstream medicine. Ann N Y Acad Sci. 2000;909:186-216. | |||||
REF 77 | Acetylmethadol metabolites influence opiate receptors and adenylate cyclase in amygdala. Eur J Pharmacol. 1981 Jul 10;72(4):343-9. | |||||
REF 78 | Antianalgesia: stereoselective action of dextro-morphine over levo-morphine on glia in the mouse spinal cord.J Pharmacol Exp Ther.2005 Sep;314(3):1101-8. | |||||
REF 79 | Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. | |||||
REF 80 | OxyContin abuse and overdose. Postgrad Med. 2009 Mar;121(2):163-7. | |||||
REF 81 | Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. | |||||
REF 82 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 319). | |||||
REF 83 | Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents. Cardiovasc Res. 1999 Dec;44(3):568-78. | |||||
REF 84 | Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71. | |||||
REF 85 | A Review of Abuse-Deterrent Opioids For Chronic Nonmalignant Pain. P T. 2012 July; 37(7): 412-418. | |||||
REF 86 | Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. | |||||
REF 87 | Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5. | |||||
REF 88 | Further studies of tyrosine surrogates in opioid receptor peptide ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. | |||||
REF 89 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight | |||||
REF 90 | The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91. | |||||
REF 91 | Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381. | |||||
REF 92 | Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. | |||||
REF 93 | Endomorphin-2: A Biased Agonist at the -Opioid Receptor. Mol Pharmacol. 2012 August; 82(2): 178-188. | |||||
REF 94 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
REF 95 | US patent application no. 6,924,288, Enantiomerically pure opioid diarylmethylpiperzine and methods of using same. | |||||
REF 96 | Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists. J Med Chem. 2008 Feb 28;51(4):1058-62. | |||||
REF 97 | Herkinorin analogues with differential beta-arrestin-2 interactions. J Med Chem. 2008 Apr 24;51(8):2421-31. | |||||
REF 98 | Novel opioid antagonists for opioid-induced bowel dysfunction. Expert Opin Investig Drugs. 2011 Aug;20(8):1047-56. | |||||
REF 99 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009073) | |||||
REF 100 | DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. II. A mixed opioid agonist with potent antinociceptive activity and limited effects on respiratory function. J Pharmacol Exp Ther. 2003 Dec;307(3):1227-33. | |||||
REF 101 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71. | |||||
REF 102 | A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo. Anesth Analg. 2005 Mar;100(3):713-7, table of contents. | |||||
REF 103 | Mirfentanil: pharmacological profile of a novel fentanyl derivative with opioid and nonopioid effects. J Pharmacol Exp Ther. 1991 Aug;258(2):502-10. | |||||
REF 104 | [3H]Sufentanil, a superior ligand for mu-opiate receptors: binding properties and regional distribution in rat brain and spinal cord. Eur J Pharmacol. 1983 Feb 18;87(2-3):209-25. | |||||
REF 105 | Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Clin Pharmacol Ther. 1994 Sep;56(3):261-71. | |||||
REF 106 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026307) | |||||
REF 107 | WO patent application no. 2007,0677,14, Treatment of sequelae of psychiatric disorders. | |||||
REF 108 | Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. | |||||
REF 109 | Inhibition of cholinergic neurotransmission in human airways by opioids. J Appl Physiol (1985). 1992 Mar;72(3):1096-100. | |||||
REF 110 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003724) | |||||
REF 111 | Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing tw... J Med Chem. 2010 Aug 12;53(15):5491-501. | |||||
REF 112 | The effects on resting ventilation of intravenous infusions of morphine or sameridine, a novel molecule with both local anesthetic and opioid properties. Anesth Analg. 1999 Jan;88(1):160-5. | |||||
REF 113 | Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. | |||||
REF 114 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem. 2006 May 18;49(10):2868-75. | |||||
REF 115 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
REF 116 | Akuammine and dihydroakuammine, two indolomonoterpene alkaloids displaying affinity for opioid receptors. J Nat Prod. 1992 Mar;55(3):380-4. | |||||
REF 117 | Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opio... J Med Chem. 2006 Jan 12;49(1):256-62. | |||||
REF 118 | 6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides. J Med Chem. 2006 Jun 15;49(12):3653-8. | |||||
REF 119 | Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists. J Med Chem. 2005 Dec 15;48(25):8035-44. | |||||
REF 120 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1. | |||||
REF 121 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2. | |||||
REF 122 | The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety. Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. | |||||
REF 123 | Discovery of novel triazole-based opioid receptor antagonists. J Med Chem. 2006 Jul 13;49(14):4044-7. | |||||
REF 124 | 14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. J Med Chem. 2009 Mar 26;52(6):1553-7. | |||||
REF 125 | Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors. J Med Chem. 2010 Jan 14;53(1):402-18. | |||||
REF 126 | Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorp... J Med Chem. 2006 Aug 24;49(17):5333-8. | |||||
REF 127 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic ... Bioorg Med Chem. 2009 Aug 15;17(16):5782-90. | |||||
REF 128 | 3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. | |||||
REF 129 | Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity. J Med Chem. 1992 May 1;35(9):1521-5. | |||||
REF 130 | Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM: Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. J Med Chem. 2000 Feb 10;43(3):381-91. | |||||
REF 131 | You HJ, Colpaert FC, Arendt-Nielsen L: The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes. Exp Neurol. 2005 Jan;191(1):174-83. | |||||
REF 132 | Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. | |||||
REF 133 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
REF 134 | Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) b... J Med Chem. 2009 Sep 24;52(18):5685-702. | |||||
REF 135 | Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-pipe... J Med Chem. 2008 Oct 9;51(19):5893-6. | |||||
REF 136 | Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. J Med Chem. 1981 Jul;24(7):903-6. | |||||
REF 137 | Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes. Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. | |||||
REF 138 | SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10. | |||||
REF 139 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-c... Bioorg Med Chem. 2008 May 15;16(10):5653-64. | |||||
REF 140 | Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. | |||||
REF 141 | Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac... Bioorg Med Chem Lett. 2006 Sep 15;16(18):4839-41. | |||||
REF 142 | Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues. Bioorg Med Chem. 2008 Apr 15;16(8):4341-6. | |||||
REF 143 | Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4946-50. | |||||
REF 144 | Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp]. J Med Chem. 2008 Sep 25;51(18):5866-70. | |||||
REF 145 | Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6. | |||||
REF 146 | Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture. J Neurochem. 1993 Feb;60(2):765-7. | |||||
REF 147 | Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. J Med Chem. 2009 Dec 10;52(23):7372-5. | |||||
REF 148 | Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine. J Med Chem. 1990 Aug;33(8):2286-96. | |||||
REF 149 | Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pha... J Med Chem. 2000 Jan 13;43(1):114-22. | |||||
REF 150 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. | |||||
REF 151 | Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. J Med Chem. 2007 Nov 1;50(22):5528-32. | |||||
REF 152 | Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis. J Med Chem. 2007 Jun 28;50(13):3138-42. | |||||
REF 153 | Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. J Biol Chem. 2007 Sep 14;282(37):27126-32. | |||||
REF 154 | Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8. | |||||
REF 155 | Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. Mol Pharmacol. 1994 Feb;45(2):330-4. | |||||
REF 156 | Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonis... J Med Chem. 2004 Jun 3;47(12):3242-7. | |||||
REF 157 | Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors. J Med Chem. 1986 Nov;29(11):2370-5. | |||||
REF 158 | Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokini... J Med Chem. 2007 Jun 14;50(12):2779-86. | |||||
REF 159 | Evaluation of N-substitution in 6,7-benzomorphan compounds. Bioorg Med Chem. 2010 Jul 15;18(14):4975-82. | |||||
REF 160 | Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opio... J Med Chem. 2006 Aug 24;49(17):5382-5. | |||||
REF 161 | Synthesis and structure-activity relationships of deltorphin analogues. J Med Chem. 1991 May;34(5):1656-61. | |||||
REF 162 | Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds. Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. | |||||
REF 163 | Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. | |||||
REF 164 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 165 | [6-O-methyl-11C]Diprenorphine Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. | |||||
REF 166 | Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mi... J Med Chem. 2007 Jun 14;50(12):2753-66. | |||||
REF 167 | Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D... J Med Chem. 2007 Feb 8;50(3):512-20. | |||||
REF 168 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1350-3. | |||||
REF 169 | Peptides as receptor selectivity modulators of opiate pharmacophores. J Med Chem. 1986 Jul;29(7):1222-5. | |||||
REF 170 | Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3. | |||||
REF 171 | Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2. Eur J Med Chem. 2010 Oct;45(10):4594-600. | |||||
REF 172 | Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4115-8. | |||||
REF 173 | Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. Br J Clin Pharmacol. 1995 Jun;39(6):611-20. | |||||
REF 174 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength Eur J Med Chem. 2008 Nov;43(11):2307-15. | |||||
REF 175 | Internalization of mu-opioid receptors produced by etorphine in the rat locus coeruleus. Neuroscience. 2001;108(3):467-77. | |||||
REF 176 | Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. | |||||
REF 177 | Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9. | |||||
REF 178 | Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1). J Med Chem. 2009 Nov 12;52(21):6941-5. | |||||
REF 179 | Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biologi... J Med Chem. 2000 Feb 24;43(4):569-80. | |||||
REF 180 | New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands. J Med Chem. 2006 Jun 29;49(13):3990-3. | |||||
REF 181 | From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. J Med Chem. 2005 Aug 25;48(17):5608-11. | |||||
REF 182 | Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists. J Med Chem. 2007 Jan 25;50(2):328-33. | |||||
REF 183 | Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic. J Med Chem. 2008 Aug 28;51(16):5109-17. | |||||
REF 184 | Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic. J Med Chem. 2004 Dec 16;47(26):6541-6. | |||||
REF 185 | Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore. J Med Chem. 2006 Sep 7;49(18):5610-7. | |||||
REF 186 | New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. | |||||
REF 187 | Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502). Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. | |||||
REF 188 | A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic. Bioorg Med Chem. 2007 Nov 15;15(22):6876-81. | |||||
REF 189 | Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity. J Med Chem. 2007 Mar 22;50(6):1414-7. | |||||
REF 190 | Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity. J Med Chem. 1991 Oct;34(10):3125-32. | |||||
REF 191 | Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors. J Med Chem. 1993 Nov 26;36(24):3748-56. | |||||
REF 192 | A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid ... J Med Chem. 2008 Mar 13;51(5):1369-76. | |||||
REF 193 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. J Med Chem. 2006 Mar 9;49(5):1773-80. | |||||
REF 194 | Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. J Med Chem. 2007 Jan 11;50(1):165-8. | |||||
REF 195 | The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues. J Med Chem. 2009 Nov 12;52(21):6814-21. | |||||
REF 196 | Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide. J Med Chem. 1994 Sep 2;37(18):2856-64. | |||||
REF 197 | Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1055-8. | |||||
REF 198 | Potential affinity labels for the opiate receptor based on fentanyl and related compounds. J Med Chem. 1982 Aug;25(8):913-9. | |||||
REF 199 | 14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid rece... J Med Chem. 2009 Nov 12;52(21):6926-30. | |||||
REF 200 | Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands. J Med Chem. 2009 Dec 10;52(23):7389-96. | |||||
REF 201 | In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. | |||||
REF 202 | Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. | |||||
REF 203 | High-affinity carbamate analogues of morphinan at opioid receptors. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. | |||||
REF 204 | New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores. J Med Chem. 2006 Sep 7;49(18):5640-3. | |||||
REF 205 | Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates a... J Med Chem. 1982 Dec;25(12):1423-7. | |||||
REF 206 | Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers. J Med Chem. 1991 Aug;34(8):2438-44. | |||||
REF 207 | Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization. Bioorg Med Chem. 2007 Feb 15;15(4):1694-702. | |||||
REF 208 | Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4978-81. | |||||
REF 209 | Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5035-8. | |||||
REF 210 | Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an ... J Med Chem. 2007 Aug 9;50(16):3765-76. | |||||
REF 211 | Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility. J Med Chem. 2008 Apr 24;51(8):2571-4. | |||||
REF 212 | Respiratory effects and tolerability of Mr 2264 Cl.A new opiate partial agonist in comparison with morphine and placebo.Eur J Clin Pharmacol.1994;46(4):301-4. | |||||
REF 213 | Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selecti... J Med Chem. 1999 Dec 30;42(26):5359-68. | |||||
REF 214 | Design and synthesis of KNT-127, a -opioid receptor agonist effective by systemic administration. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. | |||||
REF 215 | Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normo... Bioorg Med Chem. 2009 Aug 15;17(16):5983-8. | |||||
REF 216 | A topochemical approach to explain morphiceptin bioactivity. J Med Chem. 1993 Mar 19;36(6):708-19. | |||||
REF 217 | Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties. J Med Chem. 2008 Jan 10;51(1):173-7. | |||||
REF 218 | The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokin... J Med Chem. 2008 Oct 23;51(20):6334-47. | |||||
REF 219 | Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides. J Med Chem. 1997 Aug 29;40(18):2948-52. | |||||
REF 220 | Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors. J Med Chem. 1994 Jan 7;37(1):141-5. | |||||
REF 221 | Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3... Bioorg Med Chem Lett. 2006 Jul 15;16(14):3688-92. | |||||
REF 222 | Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5387-91. | |||||
REF 223 | Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling. Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. | |||||
REF 224 | Carba-analogues of fentanyl are opioid receptor agonists. J Med Chem. 2010 Apr 8;53(7):2875-81. | |||||
REF 225 | Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1847-50. | |||||
REF 226 | Molecular recognition of morphine and fentanyl by the human u-opioid receptor. Cell. 2022 Nov 10;185(23):4361-4375.e19. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.