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

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.

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

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+).

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

Desiccate at RT

[1] M. SKINGLE . GR127935: a potent and selective 5-HT1D receptor antagonist[J]. Behavioural Brain Research, 1995, 73 1: Pages 157-161. DOI: 10.1016/0166-4328(96)00089-7
[2] T SHARP  S E G  V Umbers. Effect of a selective 5-HT reuptake inhibitor in combination with 5-HT1A and 5-HT1B receptor antagonists on extracellular 5-HT in rat frontal cortex in vivo[J]. British Journal of Pharmacology, 2009, 121 5: 941-946. DOI: 10.1038/sj.bjp.0701235
[3] ALFREDO MENESES  Enrique H  José A Terrón. Effects of the 5-HT receptor antagonists GR127935 (5-HT1B/1D) and MDL100907 (5-HT2A) in the consolidation of learning[J]. Behavioural Brain Research, 1997, 89 1: Pages 217-223. DOI: 10.1016/s0166-4328(97)00055-7
[4] MOHAMMAD SHEIBANI. Sumatriptan protects against myocardial ischaemia-reperfusion injury by inhibition of inflammation in rat model.[J]. Inflammopharmacology, 2019, 27 5: 1071-1080. DOI: 10.1007/s10787-019-00586-5
[5] PEGAH DEJBAN. Protective effects of sumatriptan on ischaemia/reperfusion injury following torsion/detorsion in ipsilateral and contralateral testes of rat[J]. Andrologia, 2019, 51 9. DOI: 10.1111/and.13358