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Mepyramine maleate
Chemical Name:2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyri
dine maleate
Biological Activity:
Selective inverse agonist for the H1
receptor. Inhibits histamine induced inositol phosphate (InsP) production (log
EC50 = -7.94) and intracellular calcium mobilisation. Sequesters Gq/11 protein,
reducing its availability for other receptors associated with the same
signalling pathway.
Hill
(1990) Distribution, properties and functional characteristics of three classes
of histamine receptor. Pharmacol.Rev. 42 45. Liu et al
(1994) Does the [3H] mepyramine binding site represent the histamine
H1 receptor?Re-examination
of the histamine H2 receptor with quinine. J.Pharmacol.Exp.Ther. 268
959. Carloset 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.
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