Target Information
Target General Information | Top | |||||
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Target ID |
T78709
(Former ID: TTDS00098)
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Target Name |
5-HT 1A receptor (HTR1A)
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Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Gene Name |
HTR1A
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 5 Target-related Diseases | + | ||||
1 | Anxiety disorder [ICD-11: 6B00-6B0Z] | |||||
2 | Depression [ICD-11: 6A70-6A7Z] | |||||
3 | Hypertension [ICD-11: BA00-BA04] | |||||
4 | Migraine [ICD-11: 8A80] | |||||
5 | Mood disorder [ICD-11: 6A60-6E23] | |||||
Function |
Functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC RQ Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T31QEZ |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 8 Approved Drugs | + | ||||
1 | Buspirone | Drug Info | Approved | Anxiety disorder | [2], [3] | |
2 | Flibanserin | Drug Info | Approved | Mood disorder | [4], [5] | |
3 | OPC-34712 | Drug Info | Approved | Major depressive disorder | [6], [7] | |
4 | TERTATOLOL | Drug Info | Approved | Hypertension | [8], [9] | |
5 | Trazodone | Drug Info | Approved | Depression | [10], [11] | |
6 | Treximet | Drug Info | Approved | Migraine | [12] | |
7 | Urapidil | Drug Info | Approved | Hypertension | [9] | |
8 | Vilazodone | Drug Info | Approved | Major depressive disorder | [13], [14] | |
Clinical Trial Drug(s) | [+] 32 Clinical Trial Drugs | + | ||||
1 | CM-2395 | Drug Info | Phase 3 | Schizophrenia | [15] | |
2 | Eltoprazine | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [16] | |
3 | SEP-363856 | Drug Info | Phase 3 | Schizophrenia | [17] | |
4 | Xaliproden | Drug Info | Phase 3 | Juvenile idiopathic arthritis | [18] | |
5 | LECOZOTAN HYDROCHLORIDE | Drug Info | Phase 2/3 | Cognitive impairment | [19] | |
6 | Sarizotan | Drug Info | Phase 2/3 | Rett syndrome | [20] | |
7 | Ensaculin hydrochloride | Drug Info | Phase 2 | Parkinson disease | [21] | |
8 | FKW00GA | Drug Info | Phase 2 | Social phobia | [16] | |
9 | Mazapertine succinate | Drug Info | Phase 2 | Psychotic disorder | [22] | |
10 | MIN-117 | Drug Info | Phase 2 | Major depressive disorder | [23] | |
11 | MN-305 | Drug Info | Phase 2 | Mood disorder | [24] | |
12 | Neu-P11 | Drug Info | Phase 2 | Insomnia | [25] | |
13 | OPC-14523 | Drug Info | Phase 2 | Mood disorder | [26] | |
14 | ORG-13011 | Drug Info | Phase 2 | Psychotic disorder | [27] | |
15 | RP5063 | Drug Info | Phase 2 | Schizophrenia | [28] | |
16 | S-15535 | Drug Info | Phase 2 | Anxiety disorder | [29], [30] | |
17 | S-16924 | Drug Info | Phase 2 | Anxiety disorder | [31], [32], [33] | |
18 | SDZ-MAR-327 | Drug Info | Phase 2 | Psychotic disorder | [34], [35] | |
19 | SUN N4057 | Drug Info | Phase 2 | Coronary artery disease | [36] | |
20 | TGBA01AD | Drug Info | Phase 2 | Mood disorder | [24] | |
21 | TGFK08AA | Drug Info | Phase 2 | Generalized anxiety disorder | [37] | |
22 | TGFK09SD | Drug Info | Phase 2 | Hypoactive sexual desire dysfunction | [38] | |
23 | TGWOOAA | Drug Info | Phase 2 | Social phobia | [39] | |
24 | Zalospirone | Drug Info | Phase 2 | Anxiety disorder | [40], [41] | |
25 | 1192U90 | Drug Info | Phase 1 | Psychotic disorder | [42] | |
26 | AV-965 | Drug Info | Phase 1 | Alzheimer disease | [43] | |
27 | DSP-1053 | Drug Info | Phase 1 | Major depressive disorder | [44] | |
28 | GSK-958108 | Drug Info | Phase 1 | Premature ejaculation | [45] | |
29 | NLX-101 | Drug Info | Phase 1 | Rett syndrome | [46] | |
30 | SKL-PSY | Drug Info | Phase 1 | Bipolar disorder | [47] | |
31 | SSR-181507 | Drug Info | Phase 1 | Schizophrenia | [34] | |
32 | Umespirone | Drug Info | Phase 1 | Anxiety disorder | [48] | |
Patented Agent(s) | [+] 5 Patented Agents | + | ||||
1 | PMID30124346-Compound-13TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [49] | |
2 | PMID30124346-Compound-34TABLE4 | Drug Info | Patented | Attention deficit hyperactivity disorder | [49] | |
3 | PMID30124346-Compound-60TABLE5 | Drug Info | Patented | Parkinson disease | [49], [50], [51] | |
4 | PMID30124346-Compound-LDT66 | Drug Info | Patented | Benign prostatic hyperplasia | [49] | |
5 | PMID30124346-Compound-LDT8 | Drug Info | Patented | Benign prostatic hyperplasia | [49] | |
Discontinued Drug(s) | [+] 36 Discontinued Drugs | + | ||||
1 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | Withdrawn from market | Addictive disorder | [52], [53] | |
2 | Bifeprunox | Drug Info | Discontinued in Phase 3 | Schizophrenia | [34] | |
3 | BMS-181100 | Drug Info | Discontinued in Phase 3 | Psychotic disorder | [54], [55] | |
4 | Flesinoxan | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [56], [57] | |
5 | Adatanserin | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
6 | ALNESPIRONE | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [58] | |
7 | AP-521 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [59] | |
8 | DU 125530 | Drug Info | Discontinued in Phase 2 | Mood disorder | [60] | |
9 | GSK163090 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [61] | |
10 | LESOPITRON DIHYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Mood disorder | [62] | |
11 | PRX-00023 | Drug Info | Discontinued in Phase 2 | Mood disorder | [24] | |
12 | REC-15/3079 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [63], [64] | |
13 | Robalzotan | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [65], [66] | |
14 | BINOSPIRONE MESYLATE | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [67] | |
15 | DU-29894 | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [68] | |
16 | E2101 | Drug Info | Discontinued in Phase 1 | Spasm | [69] | |
17 | Ebalzotan | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [70] | |
18 | Eptapirone | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [71] | |
19 | GR-127607 | Drug Info | Discontinued in Phase 1 | Migraine | [72] | |
20 | Nerisopam | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [73] | |
21 | SLV-313 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [34] | |
22 | SUN-8399 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [74] | |
23 | U-93385 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [75] | |
24 | A-74283 | Drug Info | Terminated | Hypertension | [77] | |
25 | Anpirtoline | Drug Info | Terminated | Pain | [78] | |
26 | BTS-79018 | Drug Info | Terminated | Schizophrenia | [34] | |
27 | CGS-18102A | Drug Info | Terminated | Anxiety disorder | [79] | |
28 | Du-123015 | Drug Info | Terminated | Anxiety disorder | [80] | |
29 | Gepirone | Drug Info | Terminated | Depression | [24] | |
30 | HT-90B | Drug Info | Terminated | Anxiety disorder | [81] | |
31 | Ipsapirone | Drug Info | Terminated | Anxiety disorder | [82], [83] | |
32 | LY-293284 | Drug Info | Terminated | Anxiety disorder | [84], [85] | |
33 | RWJ-25730 | Drug Info | Terminated | Psychotic disorder | [86] | |
34 | S-14506 | Drug Info | Terminated | Anxiety disorder | [87], [88] | |
35 | SLV-307 | Drug Info | Terminated | Parkinson disease | [89] | |
36 | WAY-100635 | Drug Info | Terminated | Eating disorder | [90], [91] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | CM-2236 | Drug Info | Preclinical | Post-traumatic stress disorder | [76] | |
2 | PD-158771 | Drug Info | Preclinical | Schizophrenia | [34] | |
Mode of Action | [+] 7 Modes of Action | + | ||||
Agonist | [+] 50 Agonist drugs | + | ||||
1 | Buspirone | Drug Info | [1] | |||
2 | Urapidil | Drug Info | [97] | |||
3 | CM-2395 | Drug Info | [98] | |||
4 | Eltoprazine | Drug Info | [99] | |||
5 | SEP-363856 | Drug Info | [20] | |||
6 | MN-305 | Drug Info | [24] | |||
7 | Neu-P11 | Drug Info | [105] | |||
8 | SUN N4057 | Drug Info | [113] | |||
9 | Zalospirone | Drug Info | [41] | |||
10 | 1192U90 | Drug Info | [34] | |||
11 | Aryl piperazine derivative 14 | Drug Info | [49] | |||
12 | Aryl piperazine derivative 15 | Drug Info | [49] | |||
13 | Aryl piperazine derivative 16 | Drug Info | [49] | |||
14 | PMID30124346-Compound-13TABLE4 | Drug Info | [49] | |||
15 | Flesinoxan | Drug Info | [129] | |||
16 | Adatanserin | Drug Info | [24], [132] | |||
17 | ALNESPIRONE | Drug Info | [133], [9] | |||
18 | AP-521 | Drug Info | [134], [9] | |||
19 | LESOPITRON DIHYDROCHLORIDE | Drug Info | [136] | |||
20 | Ebalzotan | Drug Info | [144] | |||
21 | Eptapirone | Drug Info | [145] | |||
22 | GR-127607 | Drug Info | [146] | |||
23 | Nerisopam | Drug Info | [147] | |||
24 | SUN-8399 | Drug Info | [149] | |||
25 | U-93385 | Drug Info | [150], [9] | |||
26 | CM-2236 | Drug Info | [151] | |||
27 | A-74283 | Drug Info | [152] | |||
28 | Gepirone | Drug Info | [24] | |||
29 | Ipsapirone | Drug Info | [159] | |||
30 | LY-293284 | Drug Info | [160] | |||
31 | 1-naphthylpiperazine | Drug Info | [184], [173] | |||
32 | 5-CT | Drug Info | [199] | |||
33 | 7-methoxy-1-naphthylpiperazine | Drug Info | [184] | |||
34 | BRL-15572 | Drug Info | [203] | |||
35 | CP 93129 | Drug Info | [199] | |||
36 | EDMT | Drug Info | [206] | |||
37 | FG-5893 | Drug Info | [210] | |||
38 | L-772,405 | Drug Info | [212] | |||
39 | LP-12 | Drug Info | [213] | |||
40 | LP-211 | Drug Info | [214] | |||
41 | LP-44 | Drug Info | [213] | |||
42 | LY 165,163 | Drug Info | [210] | |||
43 | nafadotride | Drug Info | [210] | |||
44 | piribedil | Drug Info | [221] | |||
45 | S-14671 | Drug Info | [111] | |||
46 | SB 216641 | Drug Info | [203] | |||
47 | spiroxatrine | Drug Info | [210] | |||
48 | U92016A | Drug Info | [231] | |||
49 | [3H]8-OH-DPAT | Drug Info | [236] | |||
50 | [3H]NLX-112 | Drug Info | [237] | |||
Modulator | [+] 34 Modulator drugs | + | ||||
1 | Flibanserin | Drug Info | [5] | |||
2 | OPC-34712 | Drug Info | [92], [93] | |||
3 | Trazodone | Drug Info | [95] | |||
4 | Vilazodone | Drug Info | [14] | |||
5 | Sarizotan | Drug Info | [102] | |||
6 | Ensaculin hydrochloride | Drug Info | [21], [103] | |||
7 | FKB01MD | Drug Info | [16] | |||
8 | Mazapertine succinate | Drug Info | [102] | |||
9 | OPC-14523 | Drug Info | [106] | |||
10 | S-16924 | Drug Info | [32], [33] | |||
11 | SDZ-MAR-327 | Drug Info | [112] | |||
12 | TGBA01AD | Drug Info | [114] | |||
13 | TGFK08AA | Drug Info | [115] | |||
14 | TGFK09SD | Drug Info | [116] | |||
15 | NLX-101 | Drug Info | [121] | |||
16 | SKL-PSY | Drug Info | [122] | |||
17 | SSR-181507 | Drug Info | [123] | |||
18 | Bifeprunox | Drug Info | [126] | |||
19 | BMS-181100 | Drug Info | [127], [128] | |||
20 | PRX-00023 | Drug Info | [138] | |||
21 | DU-29894 | Drug Info | [142] | |||
22 | E2101 | Drug Info | [143] | |||
23 | SLV-313 | Drug Info | [148] | |||
24 | Anpirtoline | Drug Info | [78] | |||
25 | CGS-18102A | Drug Info | [155] | |||
26 | Du-123015 | Drug Info | [157] | |||
27 | HT-90B | Drug Info | [158] | |||
28 | RWJ-25730 | Drug Info | [162] | |||
29 | S-14506 | Drug Info | [163] | |||
30 | CGS-19480A | Drug Info | [204], [9] | |||
31 | EMD 56551 | Drug Info | [207] | |||
32 | NPT-500 | Drug Info | [122] | |||
33 | SEL-73 | Drug Info | [122] | |||
34 | SR-59026 | Drug Info | [230] | |||
Inhibitor | [+] 142 Inhibitor drugs | + | ||||
1 | TERTATOLOL | Drug Info | [94] | |||
2 | LYSERGIC ACID DIETHYLAMIDE | Drug Info | [125] | |||
3 | Sunepitron | Drug Info | [130] | |||
4 | TIOSPIRONE | Drug Info | [131] | |||
5 | MAZAPERTINE | Drug Info | [137] | |||
6 | A-80426 | Drug Info | [153] | |||
7 | BMY-7378 | Drug Info | [154] | |||
8 | CP-293019 | Drug Info | [156] | |||
9 | WB-4101 | Drug Info | [168] | |||
10 | (3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | [169] | |||
11 | (R)-(-)-10-methyl-11-hydroxyaporphine | Drug Info | [170] | |||
12 | (R)-11-Amino-2-methoxyaporphine | Drug Info | [171] | |||
13 | (R)-2,11-Diaminoaporphine | Drug Info | [171] | |||
14 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [173] | |||
15 | 1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane | Drug Info | [174] | |||
16 | 1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane | Drug Info | [174] | |||
17 | 1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane | Drug Info | [174] | |||
18 | 1,6-bis(4-m-tolylpiperazin-1-yl)hexane | Drug Info | [174] | |||
19 | 1,6-bis(4-phenylpiperazin-1-yl)hexane | Drug Info | [174] | |||
20 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [175] | |||
21 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [169] | |||
22 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [169] | |||
23 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [176] | |||
24 | 1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine | Drug Info | [177] | |||
25 | 1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine | Drug Info | [178] | |||
26 | 1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | [177] | |||
27 | 1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | [177] | |||
28 | 1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | [177] | |||
29 | 1-(2-(benzyloxy)phenyl)piperazine | Drug Info | [177] | |||
30 | 1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | [177] | |||
31 | 1-(2-Butoxy-phenyl)-piperazine | Drug Info | [179] | |||
32 | 1-(2-Chloro-phenyl)-piperazine | Drug Info | [180] | |||
33 | 1-(2-Ethoxy-phenyl)-piperazine | Drug Info | [179] | |||
34 | 1-(2-Fluoro-phenyl)-piperazine | Drug Info | [179] | |||
35 | 1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | [179] | |||
36 | 1-(2-Methoxy-phenyl)-4-propyl-piperazine | Drug Info | [181] | |||
37 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [180] | |||
38 | 1-(2-methoxyphenyl)-4-pentylpiperazine | Drug Info | [182] | |||
39 | 1-(2-phenoxyphenyl)piperazine | Drug Info | [177] | |||
40 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [183] | |||
41 | 1-(3-Fluoro-phenyl)-piperazine | Drug Info | [179] | |||
42 | 1-(3-Nitro-phenyl)-piperazine | Drug Info | [179] | |||
43 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [169] | |||
44 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [184] | |||
45 | 1-(benzyloxy)-2-(2-phenylethyl)benzene | Drug Info | [185] | |||
46 | 1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene | Drug Info | [185] | |||
47 | 1-Benzyl-4-chroman-2-ylmethyl-piperazine | Drug Info | [186] | |||
48 | 1-Butyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [181] | |||
49 | 1-Ethyl-4-(2-methoxy-phenyl)-piperazine | Drug Info | [181] | |||
50 | 1-Methyl-1,3-dihydro-indol-2-one | Drug Info | [187] | |||
51 | 1-Naphthalen-2-yl-piperazine | Drug Info | [173] | |||
52 | 1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [188] | |||
53 | 1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene | Drug Info | [185] | |||
54 | 2-(2'-methyl-biphenyl-3-yl)-ethylamine | Drug Info | [189] | |||
55 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [176] | |||
56 | 2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
57 | 2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
58 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
59 | 2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
60 | 2-(3-Bromophenylthio)-N,N-dimethylethanamine | Drug Info | [190] | |||
61 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
62 | 2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [186] | |||
63 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
64 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [176] | |||
65 | 2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine | Drug Info | [191] | |||
66 | 2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine | Drug Info | [192] | |||
67 | 2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine | Drug Info | [190] | |||
68 | 2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol | Drug Info | [94] | |||
69 | 2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | [178] | |||
70 | 2-Piperazin-1-yl-benzonitrile | Drug Info | [179] | |||
71 | 2-Piperazin-1-yl-phenol | Drug Info | [169] | |||
72 | 2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [185] | |||
73 | 3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole | Drug Info | [193] | |||
74 | 3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | [188] | |||
75 | 3-(2-Amino-propyl)-1H-indol-5-ol | Drug Info | [192] | |||
76 | 3-(2-Benzylamino-ethoxy)-phenol | Drug Info | [194] | |||
77 | 3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine | Drug Info | [188] | |||
78 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one | Drug Info | [186] | |||
79 | 3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one | Drug Info | [186] | |||
80 | 3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | [178] | |||
81 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [169] | |||
82 | 3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [195] | |||
83 | 3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol | Drug Info | [195] | |||
84 | 3-Naphthalen-1-yl-1-propyl-pyrrolidine | Drug Info | [188] | |||
85 | 3-Naphthalen-1-yl-pyrrolidine | Drug Info | [188] | |||
86 | 3-Phenyl-1-propyl-pyrrolidine | Drug Info | [188] | |||
87 | 3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine | Drug Info | [185] | |||
88 | 4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol | Drug Info | [196] | |||
89 | 4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | [177] | |||
90 | 4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | [177] | |||
91 | 4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
92 | 4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
93 | 4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | [177] | |||
94 | 4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
95 | 4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | [177] | |||
96 | 4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | [177] | |||
97 | 4-(2-(benzyloxy)phenyl)piperidine | Drug Info | [177] | |||
98 | 4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine | Drug Info | [178] | |||
99 | 4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
100 | 4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | [177] | |||
101 | 4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | [177] | |||
102 | 4-(2-phenoxyphenyl)piperidine | Drug Info | [177] | |||
103 | 4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | [177] | |||
104 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [197] | |||
105 | 4-Benzyl-1-chroman-2-ylmethyl-piperidine | Drug Info | [186] | |||
106 | 4-Benzyl-1-chroman-3-ylmethyl-piperidine | Drug Info | [186] | |||
107 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
108 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
109 | 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
110 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
111 | 8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine | Drug Info | [94] | |||
112 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [173] | |||
113 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [173] | |||
114 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [198] | |||
115 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [173] | |||
116 | 9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine | Drug Info | [94] | |||
117 | A-987306 | Drug Info | [201] | |||
118 | AGROCLAVINE | Drug Info | [202] | |||
119 | Brolamfetamine | Drug Info | [176] | |||
120 | CHLOROPHENYLPIPERAZINE | Drug Info | [179] | |||
121 | ESCHOLTZINE | Drug Info | [208] | |||
122 | Etisulergine | Drug Info | [209] | |||
123 | JNJ-10392980 | Drug Info | [211] | |||
124 | MCL-516 | Drug Info | [171] | |||
125 | N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine | Drug Info | [196] | |||
126 | N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine | Drug Info | [196] | |||
127 | N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide | Drug Info | [214] | |||
128 | N-methyllaurotetanine | Drug Info | [208] | |||
129 | N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide | Drug Info | [216] | |||
130 | PB-28 | Drug Info | [219] | |||
131 | PG-01037 | Drug Info | [220] | |||
132 | PHENYLPIPERAZINE | Drug Info | [173] | |||
133 | QUIPAZINE | Drug Info | [222] | |||
134 | SB-271046 | Drug Info | [227] | |||
135 | SB-656104 | Drug Info | [228] | |||
136 | SEROTONIN | Drug Info | [222] | |||
137 | SNAP-8719 | Drug Info | [229] | |||
138 | TFMPP | Drug Info | [169] | |||
139 | UH-232 | Drug Info | [232] | |||
140 | UH-301 | Drug Info | [233] | |||
141 | WAY-466 | Drug Info | [234] | |||
142 | [3H]spiperone | Drug Info | [168] | |||
Antagonist | [+] 41 Antagonist drugs | + | ||||
1 | Treximet | Drug Info | [96] | |||
2 | Xaliproden | Drug Info | [100] | |||
3 | LECOZOTAN HYDROCHLORIDE | Drug Info | [9], [101] | |||
4 | FKW00GA | Drug Info | [16] | |||
5 | MIN-117 | Drug Info | [104] | |||
6 | ORG-13011 | Drug Info | [9], [107] | |||
7 | RP5063 | Drug Info | [108], [109] | |||
8 | S-15535 | Drug Info | [9], [110], [111] | |||
9 | TGWOOAA | Drug Info | [117] | |||
10 | AV-965 | Drug Info | [118] | |||
11 | DSP-1053 | Drug Info | [119] | |||
12 | GSK-958108 | Drug Info | [120] | |||
13 | Umespirone | Drug Info | [124] | |||
14 | PMID30124346-Compound-LDT8 | Drug Info | [49] | |||
15 | DU 125530 | Drug Info | [135] | |||
16 | GSK163090 | Drug Info | [96] | |||
17 | REC-15/3079 | Drug Info | [139] | |||
18 | Robalzotan | Drug Info | [140] | |||
19 | BINOSPIRONE MESYLATE | Drug Info | [141], [9] | |||
20 | PD-158771 | Drug Info | [34] | |||
21 | NAN-190 | Drug Info | [161] | |||
22 | SDZ 216-525 | Drug Info | [161] | |||
23 | SLV-307 | Drug Info | [164] | |||
24 | WAY-100635 | Drug Info | [135], [165], [166], [167] | |||
25 | (R)-flurocarazolol | Drug Info | [172] | |||
26 | (S)-flurocarazolol | Drug Info | [172] | |||
27 | 9-OH-risperidone | Drug Info | [200] | |||
28 | cyamemazine | Drug Info | [205] | |||
29 | GR 125,743 | Drug Info | [199] | |||
30 | LY433221 | Drug Info | [215] | |||
31 | MPDT | Drug Info | [206] | |||
32 | P-MPPI | Drug Info | [217], [161] | |||
33 | p-[18F]MPPF | Drug Info | [218] | |||
34 | repinotan | Drug Info | [223] | |||
35 | SB 272183 | Drug Info | [225] | |||
36 | SB 649915 | Drug Info | [226] | |||
37 | SB 714786 | Drug Info | [226] | |||
38 | WAY 100135 | Drug Info | [161] | |||
39 | [11C]WAY100635 | Drug Info | [235] | |||
40 | [3H]p-MPPF | Drug Info | [238] | |||
41 | [3H]robalzotan | Drug Info | [239] | |||
Ligand | [+] 4 Ligand drugs | + | ||||
1 | Aryl piperazine derivative 1 | Drug Info | [49] | |||
2 | Aryl piperazine derivative 6 | Drug Info | [49] | |||
3 | PMID30124346-Compound-34TABLE4 | Drug Info | [49] | |||
4 | PMID30124346-Compound-60TABLE5 | Drug Info | [49] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | BTS-79018 | Drug Info | [34] | |||
Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
1 | RS-30199 | Drug Info | [224] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
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 |
---|---|---|---|
cAMP signaling pathway | hsa04024 | Affiliated Target |
![]() |
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
![]() |
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Serotonergic synapse | hsa04726 | Affiliated Target |
![]() |
Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
Taste transduction | hsa04742 | Affiliated Target |
![]() |
Class: Organismal Systems => Sensory system | Pathway Hierarchy |
Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 6.17E-05 |
---|---|---|---|---|---|
Closeness centrality | 1.92E-01 | Radiality | 1.33E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 1.70E+01 | Topological coefficient | 5.00E-01 | Eccentricity | 13 |
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 Transcription Factors |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | cAMP signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Serotonergic synapse | |||||
Panther Pathway | [+] 2 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | 5HT1 type receptor mediated signaling pathway | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Serotonin receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | Serotonin HTR1 Group and FOS Pathway | |||||
2 | SIDS Susceptibility Pathways | |||||
3 | Monoamine GPCRs | |||||
4 | GPCRs, Class A Rhodopsin-like | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204. | |||||
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: 36). | |||||
REF 3 | Glutamate and anxiety disorders. Curr Psychiatry Rep. 2007 Aug;9(4):278-83. | |||||
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: 8182). | |||||
REF 5 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
REF 6 | 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: 7672). | |||||
REF 7 | ClinicalTrials.gov (NCT01397786) Safety and Tolerability Study of Oral OPC-34712 as Maintenance Treatment in Adults With Schizophrenia. U.S. National Institutes of Health. | |||||
REF 8 | 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: 64). | |||||
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: 213). | |||||
REF 11 | Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39. | |||||
REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021926. | |||||
REF 13 | 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: 7427). | |||||
REF 14 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
REF 15 | Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010. | |||||
REF 16 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 17 | ClinicalTrials.gov (NCT04109950) A Clinical Study to Evaluate the Long-term Safety and Tolerability of an Investigational Drug in People With Schizophrenia. U.S. National Institutes of Health. | |||||
REF 18 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 19 | ClinicalTrials.gov (NCT00277810) Study Evaluating the Safety, Tolerability, and Efficacy of Lecozotan SR in Outpatients With Alzheimer's Disease. U.S. National Institutes of Health. | |||||
REF 20 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 21 | Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58. | |||||
REF 22 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. J Med Chem. 1998 Jun 4;41(12):1997-2009. | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037483) | |||||
REF 24 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
REF 25 | ClinicalTrials.gov (NCT01489969) Sleep Laboratory Study to Investigate the Safety and Efficacy of Neu-P11 in Primary Insomnia Patients. U.S. National Institutes of Health. | |||||
REF 26 | Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. | |||||
REF 27 | ClinicalTrials.gov (NCT00000189) Gepirone vs Placebo in Treatment of Cocaine Dependence - 3. U.S. National Institutes of Health. | |||||
REF 28 | ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health. | |||||
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: 26). | |||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002186) | |||||
REF 31 | 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: 167). | |||||
REF 32 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1998 Sep;286(3):1341-55. | |||||
REF 33 | S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1999 Mar;288(3):1002-14. | |||||
REF 34 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
REF 35 | Positron emission tomographic analysis of central dopamine D1 receptor binding in normal subjects treated with the atypical neuroleptic, SDZ MAR 327. Int J Mol Med. 1998 Jan;1(1):243-7. | |||||
REF 36 | ClinicalTrials.gov (NCT00272909) Efficacy of SUN N4057 in Subjects With Acute Ischemic Stroke and Measurable Penumbra on Magnetic Resonance Imaging (MRI). U.S. National Institutes of Health. | |||||
REF 37 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | |||||
REF 38 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | |||||
REF 39 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | |||||
REF 40 | 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: 58). | |||||
REF 41 | The serotonin 5-HT receptor agonist tandospirone improves executive function in common marmosets. Behav Brain Res. 2015 Jul 1;287:120-6. | |||||
REF 42 | 1192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42. | |||||
REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412) | |||||
REF 44 | ClinicalTrials.gov (NCT01774747) A Multiple Ascending Oral Dose Evaluation of the Safety, Tolerability, and Pharmacokinetics of DSP-1053 and Its Metabolites in Healthy Subjects and in Subjects With Major Depressive Disorder. U.S. National Institutes of Health. | |||||
REF 45 | ClinicalTrials.gov (NCT00664365) FTIH Study With GSK958108. 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 | Clinical pipeline report, company report or official report of SK Biopharmaceuticals. | |||||
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 800000698) | |||||
REF 49 | 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689. | |||||
REF 50 | mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706. | |||||
REF 51 | Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59. | |||||
REF 52 | 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: 17). | |||||
REF 53 | Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10. | |||||
REF 54 | 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: 8). | |||||
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 800000679) | |||||
REF 56 | 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: 1). | |||||
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 800001126) | |||||
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 800001421) | |||||
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 800004776) | |||||
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 800014469) | |||||
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 800026154) | |||||
REF 62 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001441) | |||||
REF 63 | 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: 74). | |||||
REF 64 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010455) | |||||
REF 65 | 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: 72). | |||||
REF 66 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006370) | |||||
REF 67 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000677) | |||||
REF 68 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001422) | |||||
REF 69 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013610) | |||||
REF 70 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006909) | |||||
REF 71 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010848) | |||||
REF 72 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531) | |||||
REF 73 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001415) | |||||
REF 74 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001433) | |||||
REF 75 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002172) | |||||
REF 76 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029346) | |||||
REF 77 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002258) | |||||
REF 78 | Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl Med Biol. 2006 Apr;33(3):325-32. | |||||
REF 79 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001927) | |||||
REF 80 | Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82. | |||||
REF 81 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003558) | |||||
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. (Ligand id: 42). | |||||
REF 83 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000695) | |||||
REF 84 | 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: 19). | |||||
REF 85 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003567) | |||||
REF 86 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001430) | |||||
REF 87 | 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: 24). | |||||
REF 88 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001368) | |||||
REF 89 | Pharmacokinetics, Pharmacodynamics and Tolerance of SLV 307 After Single Oral Administration in Healthy Male Volunteers. Clinical Pharmacology & Therapeutics. 02/1999; 65(2). | |||||
REF 90 | 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: 80). | |||||
REF 91 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002783) | |||||
REF 92 | Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9. | |||||
REF 93 | Brexpiprazole: First Global Approval.Drugs.2015 Sep;75(14):1687-97. | |||||
REF 94 | Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993). | |||||
REF 95 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 96 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | |||||
REF 97 | Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55. | |||||
REF 98 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127) | |||||
REF 99 | Clinical pipeline report, company report or official report of Jazz Pharmaceuticals. | |||||
REF 100 | Pharma & Vaccines. Product Development Pipeline. April 29 2009. | |||||
REF 101 | A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in... Clin Pharmacol Ther. 2008 Jan;83(1):86-96. | |||||
REF 102 | Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57. | |||||
REF 103 | The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. Pharmacol Biochem Behav. 1998 Jul;60(3):703-7. | |||||
REF 104 | Company report (Minerva Neurosciences),MIN-101,Schizophrenia, 6 trials completed; Once a day formulation completed , Phase IIa completed; Phase IIb enrollment ongoing and expected to continue over the last 3 quarters of 2015. | |||||
REF 105 | Clinical pipeline report, company report or official report of Neurim Pharmaceuticals. | |||||
REF 106 | Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88. | |||||
REF 107 | Antagonism of the 5-HT1A receptor stimulus in a conditioned taste aversion procedure. Eur Neuropsychopharmacol. 1999 Jun;9(4):345-9. | |||||
REF 108 | Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271 | |||||
REF 109 | EFFICACY AND SAFETY OF NOVEL DOPAMINE SEROTONIN STABILIZER RP 5063 IN ACUTE SCHIZOPHRENIA AND SCHIZOAFFECTIVE DISORDER. Schizophrenia Research Volume 153, Supplement 1, April 2014, Pages S22. | |||||
REF 110 | S 15535, a benzodioxopiperazine acting as presynaptic agonist and postsynaptic 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Br J Pharmacol. 1999 Nov;128(6):1207-14. | |||||
REF 111 | Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol. 1998 Mar;357(3):205-17. | |||||
REF 112 | DOI: 10.1038/sj.mp.4002062 | |||||
REF 113 | Experimental study of pharmacological hypothermia: enhanced neuroprotective effect of a novel 5-HT 1 A agonist SUN N4057 by the pharmacological hypothermia. No To Shinkei. 2001 Sep;53(9):853-8. | |||||
REF 114 | Company report (Fabrekramer) | |||||
REF 115 | 50 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87. | |||||
REF 116 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032503) | |||||
REF 117 | Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals. | |||||
REF 118 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412) | |||||
REF 119 | DSP-1053, a novel serotonin reuptake inhibitor with 5-HT1A partial agonistic activity, displays fast antidepressant effect with minimal undesirable effects in juvenile rats. Pharmacol Res Perspect. 2015 Jun;3(3):e00142. | |||||
REF 120 | Clinical pipeline report, company report or official report of GlaxoSmithKline. | |||||
REF 121 | In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat.Psychopharmacology (Berl).2012 May;221(2):261-72. | |||||
REF 122 | 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: 1). | |||||
REF 123 | SSR181507, a dopamine D receptor and 5-HT() receptor ligand: evidence for mixed anxiolytic- and antidepressant-like activities.Pharmacol Biochem Behav.2011 Jan;97(3):428-35. | |||||
REF 124 | The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96. | |||||
REF 125 | Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. J Med Chem. 1995 Mar 17;38(6):958-66. | |||||
REF 126 | Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Addict Biol.2012 Mar;17(2):274-86. | |||||
REF 127 | BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40. | |||||
REF 128 | The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat | |||||
REF 129 | Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission. Eur Neuropsychopharmacol. 1999 Sep;9(5):427-40. | |||||
REF 130 | An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35. | |||||
REF 131 | Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. J Med Chem. 1991 Nov;34(11):3316-28. | |||||
REF 132 | Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. J Med Chem. 1999Dec 16;42(25):5077-94. | |||||
REF 133 | Chronic alnespirone-induced desensitization of somatodendritic 5-HT1A autoreceptors in the rat dorsal raphe nucleus. Eur J Pharmacol. 1999 Jan 22;365(2-3):165-73. | |||||
REF 134 | The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16. | |||||
REF 135 | 5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide: a[11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans. J Pharmacol Exp Ther. 2002 Jun;301(3):1144-50. | |||||
REF 136 | Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 Oct;113(2):425-30. | |||||
REF 137 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2. | |||||
REF 138 | PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety.Pharmacol Biochem Behav.2009 Nov;94(1):8-15. | |||||
REF 139 | N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract. JPharmacol Exp Ther. 2001 Dec;299(3):1027-37. | |||||
REF 140 | Use of PET and the radioligand [carbonyl-(11)C]WAY-100635 in psychotropic drug development. Nucl Med Biol. 2000 Jul;27(5):515-21. | |||||
REF 141 | Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology (Berl). 2001 Nov;158(3):224-9. | |||||
REF 142 | A comparison of the neuro-endocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers. Br J Clin Pharmacol. 1995 Jan;39(1):7-14. | |||||
REF 143 | In vitro interactions between a potential muscle relaxant E2101 and human cytochromes P450. Drug Metab Dispos. 2002 Jul;30(7):805-13. | |||||
REF 144 | The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist. J Pharmacol Exp Ther. 2001 Dec;299(3):883-93. | |||||
REF 145 | The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol. 2005 Nov;19(6):609-13. | |||||
REF 146 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531) | |||||
REF 147 | Simultaneous determination of nerisopam, a novel anxiolytic agent showing polymorphic metabolism, and its N-acetyl metabolite from human plasma by a validated high performance liquid chromatographic method. J Chromatogr B Biomed Appl. 1996 Mar 29;678(1):63-72. | |||||
REF 148 | Synthesis and dual D2 and 5-HT1A receptor binding affinities of 7-piperazinyl and 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones. Med Chem. 2014;10(5):484-96. | |||||
REF 149 | Effects of SUN 8399, a potent and selective 5-HT1A agonist, on conflict behavior and ambulatory activity in mice: comparison with those of buspirone, tandospirone and diazepam. Jpn J Pharmacol. 1994 Apr;64(4):273-80. | |||||
REF 150 | Tolerance development to the vagal-mediated bradycardia produced by 5-HT1A receptor agonists. J Pharmacol Exp Ther. 1994 Nov;271(2):776-81. | |||||
REF 151 | CN patent application no. 104151292, Indole derivative or a pharmaceutically acceptable salt thereof. | |||||
REF 152 | Cardiovascular activity of A-74283, a 5-hydroxytryptamine 1A agent, in the spontaneously hypertensive rat. Pharmacology. 1998 Jan;56(1):17-29. | |||||
REF 153 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | |||||
REF 154 | 8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as busp... J Med Chem. 1996 Mar 1;39(5):1125-9. | |||||
REF 155 | Quantitative determination of CGS 18102A, a new anxiolytic, in human plasma using capillary gas chromatography/mass spectrometry. Biomed Chromatogr. 1992 Sep-Oct;6(5):244-7. | |||||
REF 156 | Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30. | |||||
REF 157 | Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82. | |||||
REF 158 | Pharmacological profile of (-)HT-90B, a novel 5-HT1A receptor agonist/5-HT2 receptor antagonist. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Nov;19(7):1201-16. | |||||
REF 159 | Chronic voluntary ethanol intake hypersensitizes 5-HT(1A) autoreceptors in C57BL/6J mice. J Neurochem. 2008 Dec;107(6):1660-70. | |||||
REF 160 | Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity. J Pharmacol Exp Ther. 1994 Sep;270(3):1270-81. | |||||
REF 161 | Influence of 5-HT1A receptor antagonism on plus-maze behaviour in mice. II. WAY 100635, SDZ 216-525 and NAN-190. Pharmacol Biochem Behav. 1997 Oct;58(2):593-603. | |||||
REF 162 | Piperazinylalkyl heterocycles as potential antipsychotic agents. J Med Chem. 1995 Oct 13;38(21):4198-210. | |||||
REF 163 | S 14506: novel receptor coupling at 5-HT(1A) receptors. Neuropharmacology. 2001 Mar;40(3):334-44. | |||||
REF 164 | Development and validation of a capillary electrophoresis method for the enantiomeric purity determination of SLV307, a basic potential antipsychotic compound. Electrophoresis. 2004 Aug;25(16):2854-9. | |||||
REF 165 | Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci. 1997;60(9):653-65. | |||||
REF 166 | Cocaine and serotonin: a role for the 5-HT(1A) receptor site in the mediation of cocaine stimulant effects. Behav Brain Res. 2001 Nov 29;126(1-2):127-33. | |||||
REF 167 | Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats. Eur J Pharmacol. 2000 Nov 10;408(1):19-23. | |||||
REF 168 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. J Med Chem. 1993 Oct 15;36(21):3161-5. | |||||
REF 169 | Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4. | |||||
REF 170 | R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30. | |||||
REF 171 | Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. Bioorg Med Chem. 2008 Jul 15;16(14):6675-81. | |||||
REF 172 | The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacology (Berl). 2001 Aug;157(1):111-4. | |||||
REF 173 | 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. | |||||
REF 174 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem. 2010 Jun 24;53(12):4803-7. | |||||
REF 175 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28. | |||||
REF 176 | 5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9. | |||||
REF 177 | Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. | |||||
REF 178 | Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. | |||||
REF 179 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. J Med Chem. 1989 May;32(5):1052-6. | |||||
REF 180 | Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. J Med Chem. 1991 Jun;34(6):1850-4. | |||||
REF 181 | Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new ... J Med Chem. 1994 Aug 19;37(17):2754-60. | |||||
REF 182 | Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6628-32. | |||||
REF 183 | The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. | |||||
REF 184 | 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8. | |||||
REF 185 | Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. J Med Chem. 2006 Nov 2;49(22):6607-13. | |||||
REF 186 | Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. J Med Chem. 2005 Jan 13;48(1):266-73. | |||||
REF 187 | Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity. Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31. | |||||
REF 188 | Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997). | |||||
REF 189 | Novel aminoethylbiphenyls as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. | |||||
REF 190 | SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. | |||||
REF 191 | 4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997). | |||||
REF 192 | A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem. 2003 Sep 11;46(19):4188-95. | |||||
REF 193 | 3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic a... J Med Chem. 1990 Aug;33(8):2087-93. | |||||
REF 194 | New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates. Bioorg Med Chem Lett. 1998 Feb 3;8(3):295-300. | |||||
REF 195 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. J Med Chem. 1992 Oct 30;35(22):3984-90. | |||||
REF 196 | Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. | |||||
REF 197 | 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 198 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. | |||||
REF 199 | Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):682-8. | |||||
REF 200 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73. | |||||
REF 201 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8. | |||||
REF 202 | Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9. | |||||
REF 203 | SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20. | |||||
REF 204 | WO patent application no. 2012,0025,83, Method for treating schizophrenia and related diseases with a combination therapy. | |||||
REF 205 | Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40. | |||||
REF 206 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | |||||
REF 207 | Diagnosis of migraine with aura, depression and anxiety from allelic variations in dopaminergic genes | |||||
REF 208 | Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in ... J Nat Prod. 2006 Mar;69(3):432-5. | |||||
REF 209 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-... J Med Chem. 1985 Oct;28(10):1540-2. | |||||
REF 210 | Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56. | |||||
REF 211 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69. | |||||
REF 212 | 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001. | |||||
REF 213 | Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. | |||||
REF 214 | Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor act... J Med Chem. 2008 Sep 25;51(18):5813-22. | |||||
REF 215 | Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23. | |||||
REF 216 | Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands. J Med Chem. 1988 Oct;31(10):1968-71. | |||||
REF 217 | p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90. | |||||
REF 218 | A 18F-MPPF PET normative database of 5-HT1A receptor binding in men and women over aging. J Nucl Med. 2005 Dec;46(12):1980-9. | |||||
REF 219 | New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. J Med Chem. 1996 Jan 5;39(1):176-82. | |||||
REF 220 | Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46. | |||||
REF 221 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. | |||||
REF 222 | Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50. | |||||
REF 223 | Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. J Pharmacol Exp Ther. 1998 Mar;284(3):1082-94. | |||||
REF 224 | Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat. Neuropharmacology. 1998 Jun;37(6):769-80. | |||||
REF 225 | SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol. 2001 Jul;133(6):797-806. | |||||
REF 226 | Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80. | |||||
REF 227 | Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. | |||||
REF 228 | Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor. Bioorg Med Chem Lett. 2005 Feb 1;15(3):747-50. | |||||
REF 229 | Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione ... J Med Chem. 2005 Apr 21;48(8):3076-9. | |||||
REF 230 | Effect of SR 59026A, a new 5-HT(1A) receptor agonist, on sexual activity in male rats. Behav Pharmacol. 1995 Apr;6(3):276-282. | |||||
REF 231 | Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther. 1994 Nov;271(2):875-83. | |||||
REF 232 | (Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997). | |||||
REF 233 | N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. J Med Chem. 1997 Apr 11;40(8):1252-7. | |||||
REF 234 | Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6. | |||||
REF 235 | [11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS. Brain. 2005 Apr;128(Pt 4):896-905. | |||||
REF 236 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10. | |||||
REF 237 | [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch Pharmacol. 2010 Oct;382(4):321-30. | |||||
REF 238 | Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15. | |||||
REF 239 | Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol. 1998 Nov 6;360(2-3):219-25. |
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