Target General Infomation
Target ID
T47768
Former ID
TTDS00126
Target Name
Mu-type opioid receptor
Gene Name
OPRM1
Synonyms
MOR-1; MOR1A; Mu opioid receptor; OPRM1
Target Type
Successful
Disease Anesthesia [ICD9: 338; ICD10: R20.0]
Asthma [ICD10: J45]
Analgesia [ICD9: 338; ICD10: R52, G89]
Cancer pain [ICD9: 140-229, 338,780; ICD10: R52, G89]
Cough [ICD9: 786.2; ICD10: R05]
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89]
Constipation [ICD9: 564; ICD10: K59.0]
Diarrhea [ICD9: 787.91; ICD10: A09, K59.1]
Diabetic neuropathy [ICD9: 250, 250.6, 356.0, 356.8; ICD10: E11.40]
Diarrhea-predominant IBS [ICD9: 564.1; ICD10: K58.0]
Gastrointestinal disease [ICD10: K00-K93]
Gastrointestinal disease; Pain [ICD9:338, 356.0, 356.8, 780; ICD10: K00-K93, G64, G90.0, R52, G89]
General anesthesia [ICD9: 338; ICD10: R20.0]
Headache [ICD9: 339, 784.0; ICD10: G43-G44, R51]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Movement disorder [ICD10: R25]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Migraine [ICD9: 346; ICD10: G43]
Mild pain [ICD10: R52, G89]
Moderate-to-severe acute pain [ICD9: 338,780; ICD10: R52, G89]
Non-small cell lung cancer [ICD10: C33-C34]
Narcotic depression [ICD9: 304.9, 311; ICD10: F19.20, F32]
Obesity [ICD9: 278; ICD10: E66]
Opiate dependence [ICD9: 304; ICD10: F11]
Opioid-induced constipation [ICD9: 564; ICD10: K59.0]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Substance dependence [ICD10: F10-F19]
Systemic pain [ICD10: R52, G89]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. The receptor for beta-endorphin.
BioChemical Class
GPCR rhodopsin
Target Validation
T47768
UniProt ID
Sequence
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Drugs and Mode of Action
Drug(s) Alfentanil Drug Info Approved Anesthesia [1], [2]
Alvimopan Drug Info Approved Gastrointestinal disease; Pain [3], [4], [5]
Anileridine Drug Info Approved Pain [6], [7]
Anileridine Hydrochloride Drug Info Approved Systemic pain [8]
Buprenorphine Drug Info Approved Pain [9], [10]
Diphenoxylate Drug Info Approved Diarrhea [11], [12]
Eluxadoline Drug Info Approved Diarrhea-predominant IBS [13], [14]
Fentanyl Drug Info Approved Analgesia [8]
Hydrocodone Drug Info Approved Pain [15], [16]
Levomethadyl Acetate Drug Info Approved Opiate dependence [17], [18]
Levopropoxyphene Napsylate Anhydrous Drug Info Approved Cough [8]
Methadyl Acetate Drug Info Approved Opiate dependence [19]
Methylnaltrexone bromide Drug Info Approved Opioid-induced constipation [3]
Morphine Drug Info Approved Chronic pain [8]
Naloxegol Drug Info Approved Opioid-induced constipation [20], [21], [8]
Naloxone Drug Info Approved Narcotic depression [22], [23]
Propoxyphene Hydrochloride Drug Info Approved Mild pain [8]
Remifentanil Drug Info Approved General anesthesia [24], [25]
Tapentadol hydrochloride Drug Info Approved Moderate-to-severe acute pain [3]
ALKS5461 Drug Info Phase 3 Major depressive disorder [26]
GRT-6005 Drug Info Phase 3 Diabetic neuropathy [27]
Low dose fentanyl Drug Info Phase 3 Pain [28]
Morphine-6-glucuronide Drug Info Phase 3 Pain [29]
Nalbuphine hydrochloride ER Drug Info Phase 3 Pain [30]
NKTR-181 Drug Info Phase 3 Pain [31]
TRK-820 Drug Info Phase 3 Discovery agent [32]
BEMA buprenorphine transmucosal Drug Info Phase 2 Migraine [33]
Carfentanil Drug Info Phase 2 Discovery agent [34]
MAL formulation Drug Info Phase 2 Opiate dependence [35]
TD-1211 Drug Info Phase 2 Opioid-induced constipation [36]
TPM-1/Morphine Drug Info Phase 2 Pain [37]
AIKO-150 Drug Info Phase 1 Opiate dependence [38]
Buccal fentanyl Drug Info Phase 1 Pain [39]
Cyt-1010 Drug Info Phase 1 Pain [40]
GBR-12909 Drug Info Phase 1 Discovery agent [41]
GSK1521498 Drug Info Phase 1 Obesity [42]
Hydromorphone prodrug Drug Info Phase 1 Pain [43]
KP-201 hydrocodone prodrug Drug Info Phase 1 Pain [44]
MCP-201 Drug Info Phase 1 Pain [45]
NOCICEPTIN Drug Info Phase 1 Headache [46]
GNTI Drug Info Preclinical Obesity [47]
LY-25582 Drug Info Preclinical Obesity [47]
ADL-5945 Drug Info Discontinued in Phase 2 Constipation [48]
BCH-2687 Drug Info Discontinued in Phase 2 Pain [49]
DPI-3290 Drug Info Discontinued in Phase 2 Pain [50]
DYNORPHIN A Drug Info Discontinued in Phase 2 Discovery agent [51], [52]
Frakefamide Drug Info Discontinued in Phase 2 Pain [49]
MIRFENTANIL HYDROCHLORIDE Drug Info Discontinued in Phase 2 Pain [53]
Transdur-sufentanil Drug Info Discontinued in Phase 2 Pain [54]
TREFENTANIL HYDROCHLORIDE Drug Info Discontinued in Phase 2 Pain [55]
ADL-7445 Drug Info Discontinued in Phase 1 Constipation [56]
Fentanyl MDTS Drug Info Discontinued in Phase 1 Pain [57]
KN-203 Drug Info Discontinued in Phase 1 Urinary incontinence [58]
VP004 Drug Info Discontinued in Phase 1 Substance dependence [59]
443C81 Drug Info Terminated Asthma [60]
BCH-150 Drug Info Terminated Gastrointestinal disease [61]
BIPHALIN Drug Info Terminated Discovery agent [62]
DBO-11 Drug Info Terminated Cancer pain [63]
DBO-17 Drug Info Terminated Cancer pain [64]
LY-255582 Drug Info Terminated Discovery agent [65]
Sameridine Drug Info Terminated Pain [66]
SB-213698 Drug Info Terminated Discovery agent [67]
SNF-9007 Drug Info Terminated Discovery agent [68]
Inhibitor (+/-)-nantenine Drug Info [69]
(+/-)-TRANS-U-50488 METHANESULFONATE Drug Info [70]
(-)-cyclorphan Drug Info [71]
(-)-eseroline Drug Info [70]
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) Drug Info [72]
1,10-bis-(Dmt-Tic-amino)decane Drug Info [73]
1,4-bis-(Dmt-Tic-amino)butane Drug Info [73]
1,6-bis-(Dmt-Tic-amino)hexane Drug Info [73]
1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane Drug Info [73]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info [74]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info [74]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info [74]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info [75]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-cyclopropylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info [74]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info [74]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info [75]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info [74]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info [76]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info [75]
1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol Drug Info [77]
1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol Drug Info [77]
14-O-phenylpropylnaltrexone Drug Info [78]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info [79]
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine Drug Info [79]
17-methyl-4'-methyldihydromorphinone Drug Info [80]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info [79]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Drug Info [81]
2-Benzylaminomethyl-3-hydroxymorphinan Drug Info [79]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info [79]
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone Drug Info [73]
3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone Drug Info [73]
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone Drug Info [73]
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone Drug Info [73]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info [82]
3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol Drug Info [83]
3-desoxy-3-carboxamidonaltrexone Drug Info [84]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info [85]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [86]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info [87]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info [88]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol Drug Info [74]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info [74]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info [85]
6-(2-benzylisoindolin-5-yloxy)nicotinamide Drug Info [89]
6-(2-phenethylisoindolin-5-yloxy)nicotinamide Drug Info [89]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info [85]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info [89]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info [89]
6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide Drug Info [85]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info [85]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info [90]
6-desoxonaltrexone Drug Info [84]
6beta-naltrexol HCl Drug Info [91]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info [92]
8-carboxamidocyclazocine Drug Info [93]
Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 Drug Info [94]
Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 Drug Info [94]
Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG Drug Info [95]
Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG Drug Info [95]
Ac-RYYRIK-K-(NH2)-YAFGYPS Drug Info [95]
Ac-RYYRIK-K-(NH2)-YRFB Drug Info [95]
Ac-YGGFL-NH2 Drug Info [96]
AKUAMMINE Drug Info [70]
AMINOFENTANYL Drug Info [97]
Antanal 1 Drug Info [98]
Antanal 2 Drug Info [98]
Benzyl derivative of M6G Drug Info [99]
Beta-funaltrexamine Drug Info [100]
BIPHALIN Drug Info [101]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info [71]
BREMAZOCINE Drug Info [102]
BUTORPHAN Drug Info [103]
C6S Drug Info [104]
CARBOXYFENTANYL Drug Info [105]
CCDC 710249, HCl salt Drug Info [84]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [106]
Clocinnamox Drug Info [78]
CODEINONE Drug Info [107]
CYCLAZOCINE Drug Info [103]
CYCLORPHAN Drug Info [103]
CYPRODIME Drug Info [108]
C[L-Ala-D-pro-L-Phe-D-trp] Drug Info [94]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info [94]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info [94]
C[L-Phe-D-pro-L-Phe-D-trp] Drug Info [94]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info [94]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] Drug Info [94]
C[L-Phe-D-pro-L-Tyr-D-trp] Drug Info [94]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Drug Info [94]
C[L-Tyr-D-pro-L-Phe-D-trp] Drug Info [94]
D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 Drug Info [109]
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) Drug Info [109]
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) Drug Info [109]
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 Drug Info [109]
DAMGO Drug Info [110]
DC6S Drug Info [104]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [111]
Delta-kappa opioid heterodimer Drug Info [112]
DELTORPHIN Drug Info [113]
DELTORPHIN-II Drug Info [114]
Deprotected cogener of M6G Drug Info [99]
DERMORPHIN Drug Info [95]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [111]
DIHYDROAKUAMMINE Drug Info [70]
Dimepheptanol Drug Info [90]
DM3A6S Drug Info [104]
DM3B6S Drug Info [104]
DM6S Drug Info [104]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info [115]
Dmt-Pro-Dmp-Phe-NH2 Drug Info [115]
Dmt-Pro-Dmt-Phe-NH2 Drug Info [115]
Dmt-Pro-Emp-Phe-NH2 Drug Info [115]
Dmt-Pro-Imp-Phe-NH2 Drug Info [115]
Dmt-Pro-Mmp-Phe-NH2 Drug Info [115]
Dmt-Pro-Phe-D-1-Nal-NH2 Drug Info [116]
Dmt-Pro-Phe-D-2-Nal-NH2 Drug Info [116]
Dmt-Pro-Phe-Phe-NH2 Drug Info [115]
Dmt-Pro-Tmp-Phe-NH2 Drug Info [115]
Dmt-Pro-Trp-D-2-Nal-NH2 Drug Info [116]
Dmt-Sar-Phe-D-2-Nal-NH Drug Info [117]
DPDPE Drug Info [110]
DYNORPHIN A Drug Info [118]
Dynorphin(1-8) Drug Info [119]
ELAEOCARPENINE Drug Info [120]
ENDOMORPHIN 2 Drug Info [121]
ENDOMORPHIN-1 Drug Info [122]
ETONITAZENE Drug Info [123]
FALCARINDIOL Drug Info [124]
FLUPERAMIDE Drug Info [125]
GBR-12909 Drug Info [126]
GUANIDINONALTRINDOLE Drug Info [127]
H-2',6'-dimethyltyrosine-Tic-OH Drug Info [128]
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH Drug Info [128]
H-Aba-ala-Gly-Phe-leu-OH Drug Info [129]
H-Aba-ala-Gly-Phe-Met-OH Drug Info [129]
H-Aba-Gly-Gly-Phe-Leu-OH Drug Info [129]
H-Aba-ser-Gly-Phe-Leu-Thr-OH Drug Info [129]
H-Apa-ala-Gly-Phe-leu-OH Drug Info [129]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info [129]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info [129]
H-Cdp-ser-Gly-Phe-Leu-Thr-OH Drug Info [129]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info [129]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info [129]
H-D-Phe-c[Cys-Tyr-DTrp-Orn-Thr-Pen]-Thr-NH2 Drug Info [98]
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [130]
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [130]
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [130]
H-Dmt-Aba-Gly-NH-CH2-Bid Drug Info [131]
H-Dmt-Aba-Gly-NH-CH2-Ph Drug Info [131]
H-Dmt-Aba-Gly-NH-Ph Drug Info [131]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 Drug Info [132]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH Drug Info [132]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 Drug Info [133]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH Drug Info [133]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 Drug Info [133]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH Drug Info [133]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 Drug Info [133]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH Drug Info [133]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 Drug Info [133]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH Drug Info [133]
H-Dmt-Tic-Asp-N(Me)-Ph Drug Info [134]
H-Dmt-Tic-Asp-NH-Bzl Drug Info [134]
H-Dmt-Tic-Asp-NH-Ph Drug Info [134]
H-Dmt-Tic-D-Asp-N(Me)-Ph Drug Info [134]
H-Dmt-Tic-D-Asp-NH-Ph Drug Info [134]
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) Drug Info [72]
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 Drug Info [135]
H-Dmt-Tic-Glu-NH2 Drug Info [135]
H-Dmt-Tic-Gly-N(Me)-Ph Drug Info [134]
H-Dmt-Tic-Gly-NH-Bzl Drug Info [134]
H-Dmt-Tic-Gly-NH-CH2-Bid Drug Info [131]
H-Dmt-Tic-Gly-NH-Ph Drug Info [134]
H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph Drug Info [136]
H-Dmt-Tic-Lys(Ac)-NH-Ph Drug Info [136]
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph Drug Info [136]
H-Dmt-Tic-Lys(Z)-NH-Ph Drug Info [136]
H-Dmt-Tic-Lys-NH-CH2-Ph Drug Info [136]
H-Dmt-Tic-Lys-NH-Ph Drug Info [136]
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H Drug Info [137]
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H Drug Info [137]
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H Drug Info [137]
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid Drug Info [136]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid Drug Info [134]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) Drug Info [134]
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) Drug Info [134]
H-Dmt-Tic-NH-CH2-Boa Drug Info [138]
H-Dmt-Tic-NH-CH2-Bta Drug Info [138]
H-Dmt-Tic-NH-CH2-CH2-NH2 Drug Info [139]
H-Dmt-Tic-NH-CH2-Imid Drug Info [138]
H-Dmt-Tic-NH-CH2-ImidPh Drug Info [138]
H-Dmt-Tic-NH-CH2-Indl Drug Info [138]
H-Dmt-Tic-NH-CH2-Indn Drug Info [138]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid Drug Info [136]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid Drug Info [136]
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid Drug Info [136]
H-Dmt-Tic-OH Drug Info [73]
H-mCpa-ala-Gly-Phe-leu-OH Drug Info [129]
H-mCpa-ser-Gly-Phe-Leu-Thr-OH Drug Info [129]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info [106]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 Drug Info [140]
H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 Drug Info [140]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info [140]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info [140]
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 Drug Info [141]
H-Tyr-c[D-Orn-Aic-Glu]-NH2 Drug Info [141]
H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 Drug Info [142]
H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 Drug Info [142]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 Drug Info [143]
H-Tyr-D-Ala-Gly-Phe-D-Leu Drug Info [144]
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac Drug Info [145]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H Drug Info [146]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info [146]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info [146]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc Drug Info [145]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info [145]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info [145]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info [145]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info [146]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 Drug Info [143]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Drug Info [143]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 Drug Info [143]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Drug Info [143]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl Drug Info [143]
H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 Drug Info [142]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info [129]
H-Tyr-Gly-Gly-Phe-Met-OH Drug Info [129]
H-Tyr-Pro-Ala-Phe-NH2 Drug Info [96]
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 Drug Info [72]
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 Drug Info [72]
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H Drug Info [139]
H-Tyr-Tic-Cha-Phe-OH Drug Info [133]
H-Tyr-Tic-Phe-Phe-OH Drug Info [133]
HERKINORIN Drug Info [147]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info [148]
Hydromorphone prodrug Drug Info [149]
ICI-199441 Drug Info [150]
KETOCYCLAZOCINE Drug Info [151]
KNT-5 Drug Info [152]
KNT-62 Drug Info [153]
KNT-63 Drug Info [153]
Leucine-enkephalin Drug Info [119]
LOFENTANIL Drug Info [154]
LY-255582 Drug Info [89]
M3A6S Drug Info [104]
M3B6S Drug Info [104]
M3IBu6S Drug Info [104]
M3P6S Drug Info [104]
M3Pr6S Drug Info [104]
M3S Drug Info [104]
M6G thiosaccharide analogue Drug Info [99]
M6S Drug Info [104]
MC-CAM Drug Info [155]
MCL-117 Drug Info [71]
MCL-139 Drug Info [71]
MCL-144 Drug Info [156]
MCL-145 Drug Info [71]
MCL-147 Drug Info [157]
MCL-149 Drug Info [157]
MCL-153 Drug Info [158]
MCL-154 Drug Info [158]
MCL-182 Drug Info [157]
MCL-183 Drug Info [157]
MCL-428 Drug Info [159]
MCL-429 Drug Info [159]
MCL-431 Drug Info [159]
MCL-432 Drug Info [159]
MCL-433 Drug Info [159]
MCL-434 Drug Info [159]
MCL-435 Drug Info [159]
MCL-443 Drug Info [159]
MCL-444 Drug Info [159]
MCL-445 Drug Info [157]
MCL-446 Drug Info [157]
MCL-447 Drug Info [157]
MCL-448 Drug Info [157]
MCL-449 Drug Info [159]
MCL-450 Drug Info [160]
MCL-451 Drug Info [160]
MCL-457 Drug Info [157]
MCL-458 Drug Info [157]
METAZOCINE Drug Info [161]
MM3A6S Drug Info [104]
MM3B6S Drug Info [104]
MORPHICEPTIN Drug Info [121]
MORPHINONE Drug Info [107]
MR-1029 Drug Info [162]
MR-1526 Drug Info [162]
MR-2034 Drug Info [151]
MR-2266 Drug Info [162]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info [79]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info [79]
N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 Drug Info [163]
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 Drug Info [163]
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 Drug Info [163]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info [79]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info [79]
N-isobutylnoroxymorphone Drug Info [164]
NalBzOH Drug Info [104]
Naltrexone-6-alpha-ol Drug Info [151]
Naltrexone-6-beta-ol Drug Info [151]
NOCICEPTIN Drug Info [165]
NORBINALTORPHIMINE Drug Info [166]
O-DESMETHYL TRAMADOL Drug Info [151]
Opioid Peptide [d-Ala(8)]Dynorphin derivative Drug Info [167]
ORIPAVINE Drug Info [107]
OXYMORPHINDOLE Drug Info [123]
Oxymorphone semicarbazone hydrochloride Drug Info [119]
PHENAZOCINE Drug Info [151]
RTI-5989-31 Drug Info [168]
SALVINORIN A Drug Info [147]
SB-0304 Drug Info [169]
SB-213698 Drug Info [170]
SL-3111 Drug Info [171]
SN-11 Drug Info [170]
SN-23 Drug Info [170]
SN-28 Drug Info [172]
SNF-9007 Drug Info [173]
SOMATOSTATIN Drug Info [109]
SPIROINDANYLOXYMORPHONE Drug Info [174]
THEBAINE Drug Info [107]
TPM-1/Morphine Drug Info [175]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [106]
TRK-820 Drug Info [153]
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 Drug Info [176]
Tyr-(R)-Aba-Gly-Phe-NH2 Drug Info [177]
Tyr-(R)-spiro-Aba-Gly-Phe-NH2 Drug Info [177]
Tyr-(S)-Aba-Gly-Phe-NH2 Drug Info [177]
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 Drug Info [177]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Ala-Gly-NMePhe Drug Info [100]
Tyr-D-Ala-Gly-Phe-Met-NH2 Drug Info [101]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Drug Info [178]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info [145]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 Drug Info [179]
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 Drug Info [180]
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 Drug Info [179]
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 Drug Info [179]
Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 Drug Info [179]
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 Drug Info [180]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [173]
Tyr-Pro-3,5Dmp-Phe-NH2 Drug Info [115]
Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 Drug Info [176]
Tyr-Pro-D-Phe-D-Pro-NH2 Drug Info [176]
Tyr-Pro-D-Phe-Pro-NH2 Drug Info [176]
Tyr-Pro-D-Phg-Phe-NH2 Drug Info [181]
Tyr-Pro-Dmp-Phe-NH2 Drug Info [115]
Tyr-Pro-Dmt-Phe-NH2 Drug Info [115]
Tyr-Pro-Emp-Phe-NH2 Drug Info [115]
Tyr-Pro-Hfe-Phe-NH2 Drug Info [181]
Tyr-Pro-Hfe-Pro-NH2 Drug Info [181]
Tyr-Pro-Imp-Phe-NH2 Drug Info [115]
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 Drug Info [176]
Tyr-Pro-L-(NMe)Phe-Pro-NH2 Drug Info [176]
Tyr-Pro-L-Phe-D-Pro-NH2 Drug Info [176]
Tyr-Pro-L-Phe-Pro-NH2 Drug Info [176]
Tyr-Pro-Mmp-Phe-NH Drug Info [115]
Tyr-Pro-Phe-Ala-Bn Drug Info [182]
Tyr-Pro-Phe-D-2-Nal-NH2 Drug Info [117]
Tyr-Pro-Phe-D-Ala-Bn Drug Info [182]
Tyr-Pro-Phe-D-Phg-NH2 Drug Info [181]
Tyr-Pro-Phe-D-Val-Bn Drug Info [182]
Tyr-Pro-Phe-Hfe-NH2 Drug Info [181]
Tyr-Pro-Phe-Phe-N(CH3)2 Drug Info [183]
Tyr-Pro-Phe-Phe-NHCH3 Drug Info [183]
Tyr-Pro-Phe-Phe-NHNH2 Drug Info [183]
Tyr-Pro-Phe-Phe-OC(CH3)3 Drug Info [183]
Tyr-Pro-Phe-Phe-OCH2CH3 Drug Info [183]
Tyr-Pro-Phe-Phe-OCH2OH Drug Info [183]
Tyr-Pro-Phe-Phe-OCH3 Drug Info [183]
Tyr-Pro-Phe-Phg-NH2 Drug Info [181]
Tyr-Pro-Phg-Phe-NH2 Drug Info [181]
Tyr-Pro-Phg-Pro-NH2 Drug Info [181]
Tyr-Pro-Tmp-Phe-NH Drug Info [115]
Tyr-Pro-Trp-D-Ala-Bn Drug Info [182]
Tyr-Pro-Trp-D-Val-Bn Drug Info [182]
Tyr-Pro-Trp-Gly-Bn Drug Info [182]
Tyr-Sar-Phe-D-2-Nal-NH2 Drug Info [117]
U-69593 Drug Info [104]
UFP-502 Drug Info [114]
UFP-512 Drug Info [114]
YAWF-NH2 Drug Info [96]
YGGWL-NH2 Drug Info [96]
YGWFL-NH2 Drug Info [96]
YPAA-NH2 Drug Info [96]
YPWA-NH2 Drug Info [96]
YRFB Drug Info [95]
ZYKLOPHIN Drug Info [148]
[D-Ala2]Met-enkephalinamide Drug Info [161]
[Dcp1]Dyn A(1-11)-NH2 Drug Info [111]
[Leu5]enkephalin Drug Info [184]
[Tyr-Pro-Phe-NH-CH2-]2 Drug Info [185]
[Tyr-Pro-Phe-NH-]2 Drug Info [185]
[Tyr-Pro-Phe-Phe-NH-CH2-]2 Drug Info [185]
[Tyr-Pro-Phe-Phe-NH-]2 Drug Info [185]
Agonist 3-Methylfentanyl Drug Info [186]
3-Methylthiofentanyl Drug Info [187]
Alfentanil Drug Info [188]
ALKS5461 Drug Info [189]
Anileridine Drug Info [190]
BCH-2687 Drug Info [191]
BEMA buprenorphine transmucosal Drug Info [192]
Buprenorphine Drug Info [193], [194]
Carfentanil Drug Info [195]
Cyt-1010 Drug Info [196]
DBO-11 Drug Info [197]
DBO-17 Drug Info [197]
Dihydromorphine Drug Info [198]
Dimethylthiambutene Drug Info [199]
Diphenoxylate Drug Info [200]
DPI-3290 Drug Info [201]
DSLET Drug Info [202]
dynorphin B Drug Info [202]
ethylketocyclazocine Drug Info [202]
Ethylmorphine Drug Info [203]
Etorphine Drug Info [204]
Fentanyl MDTS Drug Info [205]
Frakefamide Drug Info [206]
GSK1521498 Drug Info [42], [207]
KN-203 Drug Info [208]
KP-201 hydrocodone prodrug Drug Info [209]
Levomethadyl Acetate Drug Info [210]
Low dose fentanyl Drug Info [205]
MAL formulation Drug Info [211]
MCP-201 Drug Info [212]
Methadyl Acetate Drug Info [213]
MIRFENTANIL HYDROCHLORIDE Drug Info [214], [8]
Morphine-6-glucuronide Drug Info [197]
NE-2 Drug Info [202]
NKTR-181 Drug Info [215]
normorphine Drug Info [202]
NRP290 Drug Info [202]
PL017 Drug Info [216]
Remifentanil Drug Info [217]
TQ-1017 Drug Info [8]
Transdur-sufentanil Drug Info [218]
TREFENTANIL HYDROCHLORIDE Drug Info [219], [8]
Modulator 443C81 Drug Info [220]
AIKO-152 Drug Info [202]
Anileridine Hydrochloride Drug Info [221]
BCH-150 Drug Info [222]
Buccal fentanyl Drug Info
CC-408 Drug Info [202]
Eluxadoline Drug Info
Endomorphins Drug Info [202]
Fentanyl Drug Info
fentanyl (transmucosal film, pain), Auxilium Pharmaceuticals Drug Info [223]
GRT-6005 Drug Info [27]
Hydrocodone Drug Info
KIN-3031 Drug Info [202]
KRP-110 Drug Info [202]
Levopropoxyphene Napsylate Anhydrous Drug Info [221]
Methylnaltrexone bromide Drug Info [3]
Morphine Drug Info
Nalbuphine hydrochloride ER Drug Info
Naloxegol Drug Info [20], [8]
NCT-400 Drug Info [202]
NRT-300 Drug Info [202]
Propoxyphene Hydrochloride Drug Info
PTI-601 Drug Info [202]
Sameridine Drug Info [224]
SEMORPHONE HYDROCHLORIDE Drug Info
Tapentadol hydrochloride Drug Info [3]
TD-1211 Drug Info [225]
Antagonist ADC-5510 Drug Info [202]
ADL-5945 Drug Info [226]
ADL-7445 Drug Info [226]
AIKO-150 Drug Info [149]
AIKO-151 Drug Info [202]
Alvimopan Drug Info [227]
Beta-endorphin Drug Info [228]
CTAP Drug Info [216]
CTOP Drug Info [229]
Diprenorphine Drug Info [230]
GNTI Drug Info [47]
KIN-4044 Drug Info [202]
KRP-100 Drug Info [202]
LY-25582 Drug Info [47]
naloxonazine Drug Info [229]
Naloxone Drug Info [231], [232]
naltriben Drug Info [202]
PF-05 Drug Info [202]
quadazocine Drug Info [202]
[3H]diprenorphine Drug Info [229]
[3H]naloxone Drug Info [229]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Estrogen signaling pathway
Morphine addiction
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Enkephalin release
Pathway Interaction Database IL4-mediated signaling events
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways TCR Signaling Pathway
GPCRs, Class A Rhodopsin-like
Peptide GPCRs
Opioid Signalling
GPCR ligand binding
GPCR downstream signaling
References
REF 1FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075221.
REF 2(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 32008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
REF 4Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
REF 5(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 6(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 7Drug information of Anileridine, 2008. eduDrugs.
REF 8Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 9Buprenorphine for opioid dependence. J Pain Palliat Care Pharmacother. 2009;23(2):153-5.
REF 10(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 11FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040357.
REF 12(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(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 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031329)
REF 15FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088017.
REF 16(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 17FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020315.
REF 18(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 19FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020315.
REF 202014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 21(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 22Opioid 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 23(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 24FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020630.
REF 25(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 26ClinicalTrials.gov (NCT02158533) A Study of ALKS 5461 for the Treatment of Major Depressive Disorder (MDD) - the FORWARD-4 Study. U.S. National Institutes of Health.
REF 27Cebranopadol: 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 28A Phase III study to assess the clinical utility of low-dose fentanyl transdermal system in patients with chronic nonmalignant pain. Curr Med Res Opin. 2006 Aug;22(8):1493-501.
REF 29ClinicalTrials.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 30ClinicalTrials.gov (NCT00323154) Nalbuphine for the Treatment of Opioid Induced Pruritus in Children. U.S. National Institutes of Health.
REF 31ClinicalTrials.gov (NCT02362672) Efficacy and Safety Study of NKTR-181 in Opioid-Naive Subjects With Low Back Pain. U.S. National Institutes of Health.
REF 32ClinicalTrials.gov (NCT01513161) Efficacy and Safety Study of TRK-820 to Treat Conventional-treatment-resistant Pruritus in Patients Receiving Hemodialysis. U.S. National Institutes of Health.
REF 33ClinicalTrials.gov (NCT00941304) Study of BEMA Buprenorphine in the Treatment of Dental Pain. U.S. National Institutes of Health.
REF 34ClinicalTrials.gov (NCT01899170) Towards Individualized Deep Brain Stimulation Treatment of Chronic Neuropathic Pain. U.S. National Institutes of Health.
REF 35Clinical pipeline report, company report or official report of D&A Pharma.
REF 36ClinicalTrials.gov (NCT01401985) A Study of TD-1211 in Subjects With Opioid-Induced Constipation (OIC). U.S. National Institutes of Health.
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023017)
REF 38ClinicalTrials.gov (NCT00829777) Safety Study of Intravenous 6??Naltrexol (AIKO-150) in Opioid-Dependent Subjects. U.S. National Institutes of Health.
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017692)
REF 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035166)
REF 41ClinicalTrials.gov (NCT00218049) Interaction Between Vanoxerine (GBR 12909) and Cocaine in Cocaine Dependent Individuals. U.S. National Institutes of Health.
REF 42Clinical pipeline report, company report or official report of GlaxoSmithKline (2011).
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034401)
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037883)
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018011)
REF 46ClinicalTrials.gov (NCT01404091) A Study of Nociceptin/Orphanin FQ Peptide Receptor Occupancy in Healthy Subjects. U.S. National Institutes of Health.
REF 47Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030930)
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009073)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010668)
REF 51(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: 1620).
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005877)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003921)
REF 54Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015205)
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003192)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031260)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020988)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026307)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025668)
REF 60Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000227)
REF 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003724)
REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008840)
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009577)
REF 64Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009580)
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005187)
REF 66Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005282)
REF 67Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006271)
REF 68Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006885)
REF 69Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
REF 70Akuammine and dihydroakuammine, two indolomonoterpene alkaloids displaying affinity for opioid receptors. J Nat Prod. 1992 Mar;55(3):380-4.
REF 71J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
REF 72J Med Chem. 2006 Jun 15;49(12):3653-8.6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
REF 73J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
REF 74Bioorg 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 75Bioorg 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 76Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. Epub 2009 Mar 14.The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
REF 77J Med Chem. 2006 Jul 13;49(14):4044-7.Discovery of novel triazole-based opioid receptor antagonists.
REF 78J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
REF 79J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
REF 80J Med Chem. 2006 Aug 24;49(17):5333-8.Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
REF 81Bioorg Med Chem. 2009 Aug 15;17(16):5782-90. Epub 2009 Jul 18.Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.
REF 82Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. Epub 2006 Apr 24.3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
REF 83J Med Chem. 1992 May 1;35(9):1521-5.Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
REF 84Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
REF 85Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
REF 86J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential.
REF 87J Med Chem. 2009 Sep 24;52(18):5685-702.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) benzamide (ADL5747).
REF 88J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
REF 89Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
REF 90J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
REF 91Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. Epub 2009 Mar 26.Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
REF 92Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10. Epub 2010 Aug 3.SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
REF 93Bioorg Med Chem. 2008 May 15;16(10):5653-64. Epub 2008 Mar 30.Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
REF 94Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
REF 95Bioorg Med Chem Lett. 2006 Sep 15;16(18):4839-41. Epub 2006 Jun 30.Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
REF 96Bioorg Med Chem. 2008 Apr 15;16(8):4341-6. Epub 2008 Mar 4.Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
REF 97Bioorg Med Chem Lett. 2006 Sep 15;16(18):4946-50. Epub 2006 Jul 7.Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
REF 98J Med Chem. 2008 Sep 25;51(18):5866-70.Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
REF 99Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
REF 100J Med Chem. 2009 Dec 10;52(23):7372-5.Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
REF 101J Med Chem. 2010 Aug 12;53(15):5491-501.Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
REF 102J Med Chem. 1990 Aug;33(8):2286-96.Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
REF 103J Med Chem. 2000 Jan 13;43(1):114-22.Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
REF 104Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.
REF 105J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
REF 106J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.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.
REF 107J Biol Chem. 2007 Sep 14;282(37):27126-32. Epub 2007 Jul 6.Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.
REF 108J Med Chem. 2004 Jun 3;47(12):3242-7.Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
REF 109J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
REF 110Evaluation of N-substitution in 6,7-benzomorphan compounds. Bioorg Med Chem. 2010 Jul 15;18(14):4975-82. doi: 10.1016/j.bmc.2010.06.005. Epub 2010 Jun 9.
REF 111J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
REF 112J Med Chem. 2004 Jun 3;47(12):2969-72.A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers.
REF 113J Med Chem. 1991 May;34(5):1656-61.Synthesis and structure-activity relationships of deltorphin analogues.
REF 114Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. Epub 2010 Jun 25.Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
REF 115J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
REF 116J Med Chem. 2007 Feb 8;50(3):512-20.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-2-Nal(4)]endomorphin-2 (Antanal-2).
REF 117Bioorg Med Chem Lett. 2008 Feb 15;18(4):1350-3. Epub 2008 Jan 8.Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
REF 118Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71. Epub 2007 Dec 4.Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
REF 119J Med Chem. 1986 Jul;29(7):1222-5.Peptides as receptor selectivity modulators of opiate pharmacophores.
REF 120Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3. Epub 2010 Jan 22.Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
REF 121Eur J Med Chem. 2010 Oct;45(10):4594-600. Epub 2010 Jul 21.Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.
REF 122Bioorg Med Chem Lett. 2009 Aug 1;19(15):4115-8. Epub 2009 Jun 6.Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.
REF 123Eur J Med Chem. 2008 Nov;43(11):2307-15. Epub 2008 Feb 29.Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?.
REF 124Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
REF 125Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9.Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
REF 126J Med Chem. 2001 Oct 11;44(21):3391-401.From hit to lead. Analyzing structure-profile relationships.
REF 127J Med Chem. 2003 Jul 3;46(14):3127-37.Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
REF 128J Med Chem. 2009 Nov 12;52(21):6941-5.Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
REF 129Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
REF 130J Med Chem. 2000 Feb 24;43(4):569-80.Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
REF 131J Med Chem. 2006 Jun 29;49(13):3990-3.New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
REF 132J Med Chem. 2005 Aug 25;48(17):5608-11.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.
REF 133J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
REF 134J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
REF 135J Med Chem. 2004 Dec 16;47(26):6541-6.Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
REF 136J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
REF 137Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. Epub 2005 Sep 23.New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
REF 138Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
REF 139Bioorg Med Chem. 2007 Nov 15;15(22):6876-81. Epub 2007 Aug 29.A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
REF 140J Med Chem. 2007 Mar 22;50(6):1414-7. Epub 2007 Feb 22.Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
REF 141J Med Chem. 1991 Oct;34(10):3125-32.Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
REF 142J Med Chem. 1993 Nov 26;36(24):3748-56.Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
REF 143J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
REF 144J Med Chem. 2007 Jun 14;50(12):2779-86. Epub 2007 May 22.Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
REF 145J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
REF 146J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
REF 147J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
REF 148J Med Chem. 2009 Nov 12;52(21):6814-21.The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
REF 149Clinical pipeline report, company report or official report of signaturerx.
REF 150J Med Chem. 1994 Sep 2;37(18):2856-64.Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
REF 151Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
REF 152Bioorg Med Chem Lett. 2010 Feb 1;20(3):1055-8. Epub 2009 Dec 26.Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
REF 153Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. Epub 2009 Nov 13.Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
REF 154J Med Chem. 1982 Aug;25(8):913-9.Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
REF 155J Med Chem. 2009 Nov 12;52(21):6926-30.14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
REF 156J Med Chem. 2009 Dec 10;52(23):7389-96.Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
REF 157Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
REF 158Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
REF 159Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
REF 160J Med Chem. 2006 Sep 7;49(18):5640-3.New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
REF 161J Med Chem. 1982 Dec;25(12):1423-7.Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.
REF 162J Med Chem. 1991 Aug;34(8):2438-44.Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
REF 163Bioorg Med Chem. 2007 Feb 15;15(4):1694-702. Epub 2006 Dec 12.Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
REF 164Bioorg Med Chem Lett. 2008 Sep 15;18(18):4978-81. Epub 2008 Aug 12.Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
REF 165J Med Chem. 2008 Feb 28;51(4):1058-62. Epub 2008 Jan 31.Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
REF 166Bioorg Med Chem Lett. 2010 Sep 1;20(17):5035-8. Epub 2010 Jul 13.Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
REF 167J Med Chem. 2003 Sep 11;46(19):4002-8.Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
REF 168J Med Chem. 2007 Aug 9;50(16):3765-76. Epub 2007 Jul 11.Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
REF 169J Med Chem. 2008 Apr 24;51(8):2571-4. Epub 2008 Mar 28.Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
REF 170Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
REF 171J Med Chem. 1999 Dec 30;42(26):5359-68.Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.
REF 172Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. Epub 2010 Aug 21.Design and synthesis of KNT-127, a |A-opioid receptor agonist effective by systemic administration.
REF 173J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
REF 174Bioorg Med Chem. 2009 Aug 15;17(16):5983-8. Epub 2009 Jul 3.Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
REF 175Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381.
REF 176J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
REF 177J Med Chem. 2008 Jan 10;51(1):173-7. Epub 2007 Dec 7.Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
REF 178J Med Chem. 2008 Oct 23;51(20):6334-47. Epub 2008 Sep 27.The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
REF 179J Med Chem. 1997 Aug 29;40(18):2948-52.Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
REF 180J Med Chem. 1994 Jan 7;37(1):141-5.Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
REF 181Bioorg Med Chem Lett. 2006 Jul 15;16(14):3688-92. Epub 2006 May 8.Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics inthe position 3 or 4.
REF 182Bioorg Med Chem Lett. 2009 Sep 15;19(18):5387-91. Epub 2009 Jul 30.Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.
REF 183Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
REF 184J Med Chem. 2010 Apr 8;53(7):2875-81."Carba"-analogues of fentanyl are opioid receptor agonists.
REF 185Bioorg Med Chem Lett. 2005 Apr 1;15(7):1847-50.Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.
REF 186Subramanian 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 187You 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 188Concentration-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 189Abstracts 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 190Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
REF 191Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009073)
REF 192Effects of buprenorphine/naloxone in opioid-dependent humans. Psychopharmacology (Berl). 2001 Mar;154(3):230-42.
REF 193Partial versus full agonists for opioid-mediated analgesia--focus on fentanyl and buprenorphine. Acta Anaesthesiol Belg. 2002;53(3):193-201.
REF 194Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
REF 195Wax PM, Becker CE, Curry SC: Unexpected “gas” casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
REF 196Endomorphin-2: A Biased Agonist at the ?-Opioid Receptor. Mol Pharmacol. 2012 August; 82(2): 178-188.
REF 197Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71.
REF 198Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
REF 199How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 200Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8.
REF 201DPI-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. Epub 2003 Oct 8.
REF 202(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 203Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. Br J Clin Pharmacol. 1995 Jun;39(6):611-20.
REF 204Internalization of mu-opioid receptors produced by etorphine in the rat locus coeruleus. Neuroscience. 2001;108(3):467-77.
REF 205Transdermal fentanyl versus sustained release oral morphine in strong-opioid na?ve patients with chronic low back pain. Spine (Phila Pa 1976). 2005 Nov 15;30(22):2484-90.
REF 206A 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 207Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 208Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026307)
REF 209Clinical pipeline report, company report or official report of kempharm.
REF 210Methadone-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 211Clinical pipeline report, company report or official report of D&A Pharma.
REF 212US patent application no. 6,924,288, Enantiomerically pure opioid diarylmethylpiperzine and methods of using same.
REF 213Acetylmethadol metabolites influence opiate receptors and adenylate cyclase in amygdala. Eur J Pharmacol. 1981 Jul 10;72(4):343-9.
REF 214Mirfentanil: pharmacological profile of a novel fentanyl derivative with opioid and nonopioid effects. J Pharmacol Exp Ther. 1991 Aug;258(2):502-10.
REF 215A Review of Abuse-Deterrent Opioids For Chronic Nonmalignant Pain. P T. 2012 July; 37(7): 412-418.
REF 216Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8.
REF 217The pro-nociceptive effects of remifentanil or surgical injury in mice are associated with a decrease in delta-opioid receptor mRNA levels: Prevention of the nociceptive response by on-site delivery of enkephalins. Pain. 2009 Jan;141(1-2):88-96. Epub 2008 Dec 5.
REF 218[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 219Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Clin Pharmacol Ther. 1994 Sep;56(3):261-71.
REF 220Inhibition of cholinergic neurotransmission in human airways by opioids. J Appl Physiol (1985). 1992 Mar;72(3):1096-100.
REF 221Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 222Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003724)
REF 223The ChEMBL database in 2017.
REF 224The 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 225The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91.
REF 226Novel opioid antagonists for opioid-induced bowel dysfunction. Expert Opin Investig Drugs. 2011 Aug;20(8):1047-56.
REF 227Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77.
REF 228Beta-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 229Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. Mol Pharmacol. 1994 Feb;45(2):330-4.
REF 230[6-O-methyl-11C]Diprenorphine, Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. 2006 May 24 [updated 2007 May 12].
REF 231Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70.
REF 232OxyContin abuse and overdose. Postgrad Med. 2009 Mar;121(2):163-7.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.