GR127935

GR127935 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 can be used in neurological disease research[1][2].

Product Specifications

CAS Number

[148672-13-3]

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gr127935.html

Purity

99.33

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C(OC)C(N2CCN(C)CC2)=C1)C3=CC=C(C4=CC=C(C5=NOC(C)=N5)C=C4C)C=C3

Molecular Formula

C29H31N5O3

Molecular Weight

497.59

References & Citations

[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. |[3]Skingle M, et al. GR127935: a potent and selective 5-HT1D receptor antagonist. Behav Brain Res. 1996;73 (1-2) :157-61.