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GR 127935 hydrochloride

Catalog #: 1477
8 Citations Datasheet / COA / SDS
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1477/10
1477/50
GR 127935 hydrochloride | CAS No. 148642-42-6 | 5-HT1D Receptor Antagonists
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Description: Potent and selective 5-HT1B and 5-HT1D antagonist

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

Purity: ≥98%

Product Details
Citations (8)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

GR 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.

Technical Data

M.Wt:
534.06
Formula:
C29H31N5O3.HCl
Solubility:
Soluble to 100 mM in water
Purity:
≥98%
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license

Background References

  1. Pericytes impair capillary blood flow and motor function after chronic spinal cord injury
    Y Li, AM Lucas-Osma, S Black, MV Bandet, MJ Stephens, R Vavrek, L Sanelli, KK Fenrich, AF Di Narzo, S Dracheva, IR Winship, K Fouad, DJ Bennett
    Nat. Med., 2017;0(0):.
  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
  4. Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT1D receptor antagonist.
    De Vries et al.
    Br.J.Pharmacol., 1996;118:85

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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

  1. Pericytes impair capillary blood flow and motor function after chronic spinal cord injury.
    Authors: Li Et al.
    Nat Med  2017;23:733
  2. 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
  3. 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
  4. Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11.
    Authors: Eriksson Et al.
    J Clin Endocrinol Metab  2013;18:1096
  5. Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
    Authors: Baillie Et al.
    Mol Psychiatry  2012;63:362
  6. DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons.
    Authors: Masterson and Durham
    Headache  2010;50:1424
  7. 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
  8. 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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