Catalog Number: 1477
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 Activity
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.
Technical Data
  • M.Wt:
    534.06
  • Formula:
    C29H31N5O3.HCl
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    148642-42-6
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.
Additional Information
Licensing Caveats:
Sold under license
Background References
  1. Blockade of porcine carotid vascular response to sumatriptan by GR 127935, a selective 5-HT1D receptor antagonist.
    De Vries et al.
    Br.J.Pharmacol., 1996;118:85
  2. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists.
    Clitherow et al.
    J.Med.Chem., 1994;37:2253
  3. Genetic regulation of extracellular serotonin by 5-hydroxytryptamine1A and 5-hydroxytryptamine1B autoreceptors in different brain regions of the mouse.
    Knobelman et al.
    J.Pharmacol.Exp.Ther., 2001;298:1083
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GR 127935 hydrochloride include:

4 Citations: Showing 1 - 4
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  1. 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
  2. Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11.
    Authors: Eriksson Et al.
    J Clin Endocrinol Metab 2013;18:1096
  3. Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
    Authors: Baillie Et al.
    Mol Psychiatry 2012;63:362
  4. 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

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