Specific Binding of [3H]mepyramine to Histamine H1-receptors in Vascular Smooth Muscle Membranes

Overview

Journal Agents Actions

Specialty Pharmacology

Date 1983 Apr 1

PMID 6869119

Citations 5

Affiliations

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Abstract

The antagonist-sensitive binding of [3H]mepyramine to beef aortic membranes was as expected for binding to histamine H1-receptors. [3H]mepyramine binds rapidly and in saturable fashion to the specific receptor sites, specific binding reaching equilibrium in 3 min at 37 degrees C. SCATCHARD's analysis of the binding data gave a dissociation constant of 3.0 nM for the radioligand-receptor complex and maximal number of binding sites: 31 fmol/mg protein. In the competition studies histamine H1-antagonists are more potent inhibitors of radioligand binding than H2-antagonist. They inhibit [3H]mepyramine binding in the following order: mepyramine greater than triprolidine greater than promethazine much greater than cimetidine. Binding data are in correlation with the previous pharmacological studies.

Citing Articles

Molecular characterization of specific H1-receptor agonists histaprodifen and its Nalpha-substituted analogues on bovine aortic H1-receptors.

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The effect of group selective reagents N-ethylmaleimide and dithiothreitol on histamine H1-receptor binding sites in the vascular smooth muscle membranes.

carman-Krzan M Agents Actions. 1984; 14(3-4):561-5.

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Characterization of vascular histamine H1-receptors: multiple affinity states of aortic histamine H1-receptor.

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Regulation of membrane histamine H1-receptor binding sites by guanine nucleotides, mono- and divalent cations.

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Histaminergic H1-receptors in smooth muscle and endothelium of bovine thoracic aorta.

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