GR-127935 hydrochloride

Names

[ Name ]:
GR-127935 hydrochloride

[Synonym ]:
N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide,hydrochloride

Biological Activity

[Description]:

GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1B Receptor:8.5 (pKi)

5-HT1D Receptor:8.5 (pIC50)

[References]

[1]. J W Clitherow, et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists. J Med Chem. 1994 Jul 22;37(15):2253-7.

[2]. Mohammad Nasehi, et al. Possible involvement of CA1 5-HT1B/1D and 5-HT2A/2B/2C receptors in harmaline-induced amnesia. Pharmacol Biochem Behav. 2014 Oct;125:70-77.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₂ClN₅O₃

[ Molecular Weight ]:
534.04900

[ Exact Mass ]:
533.21900

[ PSA ]:
83.73000

[ LogP ]:
5.91100

MSDS

Click to get detail MSDS

Related Compounds

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