GR 127935 hydrochloride

Catalog # Availability Size / Price Qty
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)
Supplemental Products

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

Soluble to 100 mM in water
Desiccate at RT

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

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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


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