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Submit ReviewMepyramine 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 40.15 | 100 | |
DMSO | 40.15 | 100 |
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.
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 |
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
If you know of a relevant reference for Mepyramine maleate, please let us know.
关键词: Mepyramine maleate, Mepyramine maleate supplier, Selective, H1, inverse, agonists, Receptors, Histamine, histaminergic, Pyrilamine, maleate, 0660, Tocris Bioscience
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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