N-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1-biphenyl-4-carboxamide hydrate hydrochloride

Description

GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT_1B, 5-HT_1Dα, and 5-HT_1Dβ (IC₅₀s = 3.16, 1.26, and 0.13 nM, respectively). It is selective for the 5-HT_1B and 5-HT_1D receptors over other 5-HT receptors (IC₅₀s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine . It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg. It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.

Uses

GR 127935 Hydrochloride is a selective and potent 5-HT1B/1D serotonin receptor antagonist.

Definition

ChEBI: GR 127935 hydrochloride is a hydrochloride obtained by reaction of GR 127935 with one equivalent of hydrochloric acid. Potent and selective 5-HT1B/1D receptor 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. It has a role as a serotonergic antagonist. It contains a GR 127935(1+).

Biochem/physiol Actions

Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.

storage

Desiccate at RT