GR127935

GR127935 is a **potent, selective antagonist of the serotonin receptors 5-HT1B and 5-HT1D**, used extensively in research as a pharmacological tool[1][2][3][4][5]. It demonstrates very high affinity for these receptors and displays >100-fold selectivity over other serotonin receptor subtypes, such as 5-HT1A, 5-HT2A, and 5-HT2C[2]. Its activity completely blocks functional responses mediated by 5-HT1B/D agonists, such as sumatriptan, in animal studies[1]. While primarily selective, at high concentrations it possesses moderate 5-HT2A receptor antagonism[1]. GR127935 is active in vivo (animal models) via intravenous or oral administration, and has been shown to block MDMA-induced hyperactivity and reduce drug-seeking behavior in cocaine addiction models[3][5]. It is not used clinically and is available for research purposes only[4]; it is commonly produced and distributed by chemical suppliers for laboratory use. Its full chemical name is N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide hydrochloride[2][4].

Other names

GR127935 hydrochlorideGR-127935 hydrochlorideGR 127935 hydrochloride