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Biological Activity 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.
Technical Data for Mepyramine maleate
|Storage||Store at RT|
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 Data for Mepyramine maleate
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Mepyramine maleate
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
Product Datasheets for Mepyramine maleate
References for Mepyramine maleate
References are publications that support the biological activity of the product.
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.
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Keywords: Mepyramine maleate, Mepyramine maleate supplier, Selective, H1, inverse, agonists, Receptors, Histamine, histaminergic, Pyrilamine, maleate, 0660, Tocris Bioscience
5 Citations for Mepyramine maleate
Citations are publications that use Tocris products. Selected citations for Mepyramine maleate include:
Connelly et al (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157 55 PMID: 19413571
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
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
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
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Literature in this Area
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