GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively). It is selective for the 5-HT1B and 5-HT1D 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.
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