GR 127935 hydrochloride

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Cat.No. 1477 - GR 127935 hydrochloride | C29H31N5O3.HCl | CAS No. 148642-42-6
Description: Potent, selective 5-HT1B/1D 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: ≥99% (HPLC)
Datasheet
Citations (4)
Literature

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
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 148642-42-6
PubChem ID 11497466
InChI Key SRVVUYIJVBLEJI-UHFFFAOYSA-N
Smiles Cl.COC1=C(C=C(NC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2C)C2=NOC(C)=N2)C=C1)N1CCN(C)CC1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 49.76 100

Preparing Stock Solutions

The following data is based on the product molecular weight 534.06. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.36 mL 18.72 mL
5 mM 0.37 mL 1.87 mL 3.74 mL
10 mM 0.19 mL 0.94 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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4 Citations for GR 127935 hydrochloride

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

Eriksson et al (2013) Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11. J Clin Endocrinol Metab 18 1096 PMID: 23032875

Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. Mol Psychiatry 63 362 PMID: 22691374

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.

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GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

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5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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