GR127935 (hydrochloride)

GR127935 hydrochloride is a selective and orally active 5-HT_1D and 5-HT_1B receptor antagonist with pK_i values of 8.5 for both receptors. GR127935 hydrochloride impairs memory acquisition and Serotonin (HY-B1473A)-mediated vasodilation. GR127935 hydrochloride can be used for research on amnesia, neuroendocrine cancer, and migraine^[1][2][3]. In Vitro:GR127935 (0.1 μM; 30 min) hydrochloride impairs serotonin-mediated vasodilation in isolated mesenteric arteries from VEH J:Nu nude mice, but does not impair vasodilation from BON-1 NET tumor-bearing mice^[2].
GR127935 hydrochloride is a potent and selective 5-HT_1D receptor antagonist with a pK_i of 8.5 at guinea pig striatal 5-HT_1D receptors, exhibiting 100-fold selectivity over 5-HT_1A and 5-HT_2C receptors^[3].
GR127935 (1-10 nM) hydrochloride effectively antagonizes Sumatriptan (HY-B0121B)-induced contraction of isolated canine saphenous vein at 1 and 10 nM^[3]. In Vivo:GR127935 (0.005 ng/mouse; intra-CA1) hydrochloride hydrochloride improves amnesia induced by harmaline (1 mg/kg, i.p.) in mice^[1].
GR127935 (0.005-0.5 ng/mouse; intra-CA1) hydrochloride exerts an amnesic effect on memory acquisition at 0.05 and 0.5 ng/mouse, whereas 0.005 ng/mouse is subthreshold, without affecting locomotor activity or tail flick in mice^[1].