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. 1978 Dec;75(12):6290–6294. doi: 10.1073/pnas.75.12.6290

Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramine.

V T Tran, R S Chang, S H Snyder
PMCID: PMC393167  PMID: 282646

Abstract

The antihistamine [3H]mepyramine binds to H1 histamine receptors in mammalian brain membranes. Potencies of H1 antihistamines at the binding sites correlate with their pharmacological antihistamine effects in the guinea pig ileum. Specific [3H]mepyramine binding is saturable with a dissociation constant of about 4 nM in both equilibrium and kinetic experiments and a density of 10 pmol per gram of whole kinetic experiments and a density of 10 pmol per gram of whole brain. Some tricyclic antidepressants are potent inhibitors of specific [3H]mepyramine binding. Regional variations of [3H]mepyramine binding do not correlate with variations in endogeneous histamine and histidine decarboxylase activity.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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