GR 127935 hydrochloride

Name: GR 127935 hydrochloride
Brand: Tocris Bioscience
SKU: 1477
Price: 246 USD

Tocris Bioscience a Bio-Techne Brand

Catalog # 1477

Citations (8)

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Key Product Details

Description:	Potent and selective 5-HT_1B and 5-HT_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)
Molecular Weight:	534.06

View Full Technical Details for GR 127935 hydrochloride

Biological Activity for GR 127935 hydrochloride

GR 127935 hydrochloride is a potent and selective 5-HT_1B/1D receptor antagonist (pK_i values are 8.5 for both guinea pig 5-HT_1D and rat 5-HT_1B receptors). Displays > 100-fold selectivity over 5HT_1A, 5-HT_2A, 5-HT_2C receptors and other receptor types. Centrally active following oral administration.

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Technical Data for GR 127935 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GR 127935 hydrochloride

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

Preparing Stock Solutions for GR 127935 hydrochloride

The following data is based on the product molecular weight 534.06.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References for GR 127935 hydrochloride

References are publications that support the biological activity of the product.

Knobelman Genetic regulation of extracellular serotonin by 5-hydroxytryptamine_1A and 5-hydroxytryptamine_1B autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 2001 PMID: 11504805
De Vries Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT_1D receptor antagonist. Br.J.Pharmacol. 1996 PMID: 8733580
Clitherow Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT_1D antagonists. J.Med.Chem. 1994 PMID: 8057272

Citations for GR 127935 hydrochloride (8)

Showing 1 - 8 of 8 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for GR 127935 hydrochloride include:

Li et al. (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med. 23:733
PMID: 28459438
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
Akerman et al. (2013) Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine. J Neurosci. 33:14869
PMID: 24027286
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
Masterson and Durham (2010) DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons. Headache. 50:1424
PMID: 20561068
Morikawa et al. (2006) Antimigraine drug, zolmitriptan, inhibits high-voltage activated calcium currents in a population of acutely dissociated rat trigeminal sensory neurons. Mol Pain. 2:10
PMID: 16549032

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Product Documents for GR 127935 hydrochloride

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.