A 5-HT1B and 5-HT1D receptor antagonist (IC50s = 3.16

GR127935 (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
148642-42-6
Storage:
-20
UN-No:
Non-Hazardous - /

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).{53337} 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 (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}  

 

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Description

A 5-HT1B and 5-HT1D receptor antagonist (IC50s = 3.16, 1.26, and 0.13 nM, respectively); selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays); enhances memory consolidation in an autoshaping learning task in rats when administered post-training at 10 mg/kg; has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan

Formal name: 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, monohydrochloride

Synonyms: 

Molecular weight: 534.1

CAS: 148642-42-6

Purity: ≥98%

Formulation: A crystalline solid

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