GR-127935

Details

Stereochemistry	ACHIRAL
Molecular Formula	C29H31N5O3
Molecular Weight	497.5881
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC=C(NC(=O)C2=CC=C(C=C2)C3=CC=C(C=C3C)C4=NOC(C)=N4)C=C1N5CCN(C)CC5

InChI

InChIKey=YDBCEBYHYKAFRX-UHFFFAOYSA-N

InChI=1S/C29H31N5O3/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,31,35)

HIDE SMILES / InChI

Approval Year

Targets

Primary Target	Pharmacology	Potency
5-hydroxytryptamine receptor 1D 18 Target ID: Q60484 Gene ID: 1.00379624E8 Gene Symbol: HTR1D Target Organism: Cavia porcellus (Guinea pig) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8057272	Antagonist 2849	8.5 null [pKi]
Serotonin 1b (5-HT1b) receptor 45 Target ID: CHEMBL3459 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8057272	Antagonist 2849	8.5 null [pKi]
5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 1 Target ID: 1.00009464E8 Gene Symbol: HTR2A Sources: https://www.ncbi.nlm.nih.gov/pubmed/8057272	Antagonist 2849	6.4 null [pKi]
Serotonin 1a (5-HT1a) receptor 177 Target ID: CHEMBL273 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8057272	Binding Agent 1076	6.5 null [pKi]
Serotonin 1 receptors; 5-HT1B & 5-HT1D 4 Target ID: CHEMBL2095230 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7617149\| https://www.ncbi.nlm.nih.gov/pubmed/9048762\| https://www.ncbi.nlm.nih.gov/pubmed/18952090	Antagonist 2849	141.0 nM [EC50]

PubMed

Title	Date	PubMed
A cell protection screen reveals potent inhibitors of multiple stages of the hepatitis C virus life cycle.	2010-02-23	20142494
Pharmacological profile of the inhibition by dihydroergotamine and methysergide on the cardioaccelerator sympathetic outflow in pithed rats.	2009-06-10	19356724
Progesterone reduces the effect of the serotonin 1B/1D receptor antagonist, GR 127935, on lordosis behavior.	2009-01	18952090
Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats.	2008-11-12	19211971
Activation of the 5-HT1B/D receptor reduces hindlimb neurogenic inflammation caused by sensory nerve stimulation and capsaicin.	2008-01	17499925
5-HT7 receptor-mediated dilatation in the middle meningeal artery of anesthetized rats.	2007-03-29	17316605
Potential vascular alpha1-adrenoceptor blocking properties of an array of 5-HT receptor ligands in the rat.	2006-03-27	16545797
Differential effects of 5-HT2C receptor ligands on place conditioning and locomotor activity in rats.	2005-05-16	15896731
[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties.	2005-03	15900510
The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action.	2005-02	15720791
Effect of combined administration of 5-HT1A or 5-HT1B/1D receptor antagonists and antidepressants in the forced swimming test.	2004-03-08	15033385
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004-01-30	14715155
Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization.	2002-04	11888550
Pharmacological studies of the acute effects of (+)-3,4-methylenedioxymethamphetamine on locomotor activity: role of 5-HT(1B/1D) and 5-HT(2) receptors.	2002-01	11751031
Role of 5-hydroxytryptamine1B receptors and 5-hydroxytryptamine uptake inhibition in the cocaine-evoked discriminative stimulus effects in rats.	2001-06	11453104
A61603-induced vasoconstriction in porcine carotid vasculature: involvement of a non-adrenergic mechanism.	2001-04-13	11334851
Effect of serotonin (5-HT)1B receptor ligands on cocaine sensitization in rats.	2001-04	11396515
Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor.	1999-09-10	10513577
RU-24969 disrupts d-amphetamine self-administration and responding for conditioned reward via stimulation of 5-HT1B receptors.	1999-03	10780831
SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.	1998-09	9776361
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.	1998-04-09	9548813
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.	1997-11-21	9397179
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.	1997-09	9303567
Interactions of GR127935, a 5-HT(1B/D) receptor ligand, with functional 5-HT receptors.	1997-04	9109356
Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors.	1997-03-05	9085055
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.	1996-12	8967979
GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors.	1996-10-31	8957260

Patents

Name

Type

Language

(1,1'-BIPHENYL)-4-CARBOXAMIDE, N-(4-METHOXY-3-(4-METHYL-1-PIPERAZINYL)PHENYL)-2'-METHYL-4'-(5-METHYL-1,2,4-OXADIAZOL-3-YL)-

Preferred Name

English

GR-127935

Common Name

English

Code System Code Type Description

CHEBI

64114