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.
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All Tocris products are intended for laboratory research use only.
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.
Distribution, properties and functional characteristics of three classes of histamine receptor.
Does the [3H] mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H2 receptor with quinine.
Liu et al.
The citations listed below are publications that use Tocris products. Selected citations for Mepyramine maleate include:
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