Mepyramine maleate
Chemical Name: 2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
Biological Activity
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
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.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Mepyramine, a histamine H1 receptor inverse agonist, binds perferentially to a G protein-coupled form of the receptor and sequesters G protein.
Carlos et al.
J.Biol.Chem., 2004;279:34431 -
Distribution, properties and functional characteristics of three classes of histamine receptor.
Hill
Pharmacol.Rev., 1990;42:45 -
Does the [3H] mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H2 receptor with qine
Liu et al.
J.Pharmacol.Exp.Ther., 1994;268:959
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Citations for Mepyramine maleate
The citations listed below are publications that use Tocris products. Selected citations for Mepyramine maleate include:
5 Citations: Showing 1 - 5
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A split luciferase-based probe for quantitative proximal determination of Gαq signalling in live cells.
Authors: Littmann Et al.
Sci Rep 2018;8:17179
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Involvement of H1 and H2 receptors and soluble guanylate cyclase in histamine-induced relaxation of rat mesenteric collecting lymphatics.
Authors: Kurtz Et al.
Microcirculation 2014;21:593
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The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.
Authors: Connelly Et al.
Br J Pharmacol 2009;157:55
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Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP.
Authors: Flamand Et al.
Br J Pharmacol 2004;141:552
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Mast cells are required for experimental oral allergen-induced diarrhea.
Authors: Brandt Et al.
J Clin Invest 2003;112:1666
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