GR 127935 hydrochloride

Cat. No. 1477 8 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective 5-HT_1B and 5-HT_1D antagonist

化学名： 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

纯度： ≥98% (HPLC)

引用文献 (8)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

许可信息

Sold under license

技术数据 for GR 127935 hydrochloride

分子量	534.06
公式	C₂₉H₃₁N₅O₃.HCl
储存	Desiccate at RT
纯度	≥98% (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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for GR 127935 hydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	water	49.76	100

制备储备液 for GR 127935 hydrochloride

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for GR 127935 hydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GR 127935 hydrochloride

参考文献是支持产品生物活性的出版物。

Clitherow et al (1994) Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT_1D antagonists. J.Med.Chem. 37 2253 PMID: 8057272

De Vries et al (1996) Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT_1D receptor antagonist. Br.J.Pharmacol. 118 85 PMID: 8733580

Knobelman et al (2001) 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. 298 1083 PMID: 11504805

If you know of a relevant reference for GR 127935 hydrochloride, please let us know.

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8 篇 GR 127935 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GR 127935 hydrochloride 的部分引用包括：

Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438

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

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

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

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

Masterson and Durham (2010) DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons. Headache 50 1424 PMID: 20561068

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

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