Mepyramine maleate

Pricing Availability   Qty
说明: Selective H1 inverse agonist
别名: Pyrilamine maleate
化学名: 2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
说明书
引用文献 (5)
评论
文献 (1)

生物活性 for Mepyramine maleate

Mepyramine maleate is a selective inverse agonist for the H1 receptor. Inhibits histamine induced inositol phosphate (InsP) production (log EC50 = -7.94) and intracellular calcium mobilization. Sequesters Gq/11 protein, reducing its availability for other receptors associated with the same signaling pathway.

技术数据 for Mepyramine maleate

分子量 401.46
公式 C17H23N3O.C4H4O4
储存 Store at RT
CAS Number 59-33-6
PubChem ID 5284451
InChI Key JXYWFNAQESKDNC-BTJKTKAUSA-N
Smiles OC(=O)\C=C/C(O)=O.COC1=CC=C(CN(CCN(C)C)C2=CC=CC=N2)C=C1

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 Mepyramine maleate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 40.15 100
DMSO 40.15 100

制备储备液 for Mepyramine maleate

以下数据基于产品分子量 401.46。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.49 mL 12.45 mL 24.91 mL
5 mM 0.5 mL 2.49 mL 4.98 mL
10 mM 0.25 mL 1.25 mL 2.49 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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产品说明书 for Mepyramine maleate

参考文献 for Mepyramine maleate

参考文献是支持产品生物活性的出版物。

Carlos et al (2004) Mepyramine, a histamine H1 receptor inverse agonist, binds perferentially to a G protein-coupled form of the receptor and sequesters G protein. J.Biol.Chem. 279 34431 PMID: 15192105

Hill (1990) Distribution, properties and functional characteristics of three classes of histamine receptor. Pharmacol.Rev. 42 45 PMID: 2164693

Liu et al (1994) Does the [3H] mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H2 receptor with qine J.Pharmacol.Exp.Ther. 268 959 PMID: 8114011


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关键词: Mepyramine maleate, Mepyramine maleate supplier, Selective, H1, inverse, agonists, Receptors, Histamine, histaminergic, Pyrilamine, maleate, 0660, Tocris Bioscience

5 篇 Mepyramine maleate 的引用文献

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

Connelly et al (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157 55 PMID: 19413571

Kurtz et al (2014) Involvement of H1 and H2 receptors and soluble guanylate cyclase in histamine-induced relaxation of rat mesenteric collecting lymphatics. Microcirculation 21 593 PMID: 24702851

Littmann et al (2018) A split luciferase-based probe for quantitative proximal determination of Gαq signalling in live cells. Sci Rep 8 17179 PMID: 30464299

Flamand et al (2004) Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP. Br J Pharmacol 141 552 PMID: 14744809

Brandt et al (2003) Mast cells are required for experimental oral allergen-induced diarrhea. J Clin Invest 112 1666 PMID: 14660743


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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.