GR 127935 hydrochloride
Chemical 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 hydrochloride
Biological ActivityGR 127935 hydrochloride is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists.
Clitherow et al.
Genetic regulation of extracellular serotonin by 5-hydroxytryptamine1A and 5-hydroxytryptamine1B autoreceptors in different brain regions of the mouse.
Knobelman et al.
Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT1D receptor antagonist.
De Vries et al.
Citations for GR 127935 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for GR 127935 hydrochloride include:
8 Citations: Showing 1 - 8
Pericytes impair capillary blood flow and motor function after chronic spinal cord injury.
Authors: Li Et al.
Nat Med 2017;23:733
Lasting neurobehavioral abnormalities in rats after neonatal activation of serotonin 1A and 1B receptors: possible mechanisms for serotonin dysfunction in autistic spectrum disorders.
Authors: Khatri Et al.
Psychopharmacology (Berl) 2014;231:1191
Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine.
Authors: Akerman Et al.
J Neurosci 2013;33:14869
Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11.
Authors: Eriksson Et al.
J Clin Endocrinol Metab 2013;18:1096
Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
Authors: Baillie Et al.
Mol Psychiatry 2012;63:362
DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons.
Authors: Masterson and Durham
JNK regulates serotonin-mediated proliferation and migration of pulmonary artery smooth muscle cells.
Authors: Wei Et al.
Am J Physiol Lung Cell Mol Physiol 2010;298:L863
Antimigraine drug, zolmitriptan, inhibits high-voltage activated calcium currents in a population of acutely dissociated rat trigeminal sensory neurons.
Authors: Morikawa Et al.
Mol Pain 2006;2:10
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