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GR 127935 hydrochloride
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Chemical Name:N-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methy
l-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-ca
rboxamide hydrochloride
Biological Activity:
Potent and selective 5-HT1B/1Dreceptor antagonist (pKi
values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B
receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A,
5-HT2C receptors and other receptor types. Centrally active
following oral administration.
Clitherowet al
(1994) Evolution of a novel series of [(N,N-dimethylamino)propyl]-
and piperazinylbenzalides as the first selective 5-HT1D antagonists.
J.Med.Chem. 37 2253. De Vrieset al (1996) Blockade
of porcine carotid vascular response to sumatriptan by GR 127935, a selective
5-HT1D receptor antagonist. Br.J.Pharmacol. 118 85. Knobelmanet al (2001) Genetic regulation of extracellular serotonin by
5-hydroxytryptamine1A and 5-hydroxytryptamine1B
autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 298
1083.
Atypical antipsychotic agent that displays 5-HT2A receptor antagonism. Also displays high affinity at D2 receptors (Ki values are 0.4 and 3.13 nM for 5-HT2A and D2 receptors respectively).
