GR 127935 hydrochloride

Cat. No. 1477

GR 127935 hydrochloride C29H31N5O3.HCl [148642-42-6]

Price and Availability

For GR 127935 hydrochloride pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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.

Licensing Information

Sold under license

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View 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.

If you know of a relevant reference for this product please let us know.

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.

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.

Do you know of a great paper that uses GR 127935 hydrochloride from Tocris? If so please let us know.

View Related Products by Target

View Related Products by Product Action

Keywords: GR 127935 hydrochloride, supplier, Potent, selective, 5-HT1B/1D, antagonist, Serotonin, Receptors, GR127935, hydrochloride, Tocris Bioscience, 5-HT1D Receptor Antagonist products

Quick Order

Find multiple products by catalog number

divider line

GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs Request copy or view PDF today.

divider line

5-HT Review

Written by N. Barnes & J. Neumaler

5-HT Receptors Scientific Review

Our 5-HT review summarizes the serotonin receptor subtypes and highlights their importance in mediating various physiological & pharmacological processes. Request copy or view PDF today.

divider line

LinkedIn Updates

Follow Tocris on LinkedIn

Follow us on LinkedIn!

Visit our LinkedIn page for the latest Tocris news, events and updates.