GR 127935 hydrochloride
Cat. No. 1477
Chemical Name: N-[4-Methoxy-3-(4-methyl-1-piperazi
Biological ActivityPotent 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.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Knobelman et al (2001) Genetic regulation of extracellular serotonin by 5-hydroxytryptamine1A and 5-hydroxytryptamine1B autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 298 1083. PMID: 11504805.
De Vries et al (1996) Blockade of porcine carotid vascular response to sumatriptan by GR 127935, a selective 5-HT1D receptor antagonist. Br.J.Pharmacol. 118 85. PMID: 8733580.
Clitherow et al (1994) Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J.Med.Chem. 37 2253. PMID: 8057272.
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Citations are publications that use Tocris products. Selected citations for GR 127935 hydrochloride include:
Khatri et al (2014) Lasting neurobehavioral abnormalities in rats after neonatal activation of serotonin 1A and 1B receptors: possible mechanisms for serotonin dysfunction in autistic spectrum disorders. Psychopharmacology (Berl) 231 1191. PMID: 23975037.
Eriksson et al (2013) Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11. J Clin Endocrinol Metab 18 1096. PMID: 23032875.
Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. Mol Psychiatry 63 362. PMID: 22691374.
Wei et al (2010) JNK regulates serotonin-mediated proliferation and migration of pulmonary artery smooth muscle cells. Am J Physiol Lung Cell Mol Physiol 298 L863. PMID: 20228179.
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