The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Antimuscarinic Effects of Antihistamines: Quantitative Evaluation by Receptor-Binding Assay
Nobuo KUBOOsamu SHIRAKAWATakayoshi KUNOChikako TANAKA
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1987 Volume 43 Issue 3 Pages 277-282

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Abstract

Quantitative evaluation of antimuscarinic effects of antihistamines (H1and H2-receptor antagonists) was carried out using a receptor-binding assay. The inhibition constants (K1 values) of twenty seven H1-receptor antagonists, one related antidepressant and three H2-receptor antagonists at H1-receptors and muscarinic receptors in the bovine cerebral cortex were determined. All the H2receptor antagonists examined showed very low affinity for the muscarinic receptors. On the other hand, some H1-receptor antagonists (mequitazine, cyproheptazine, clemastine, diphenylpyraline, promethazine, homochlorcyclizine and alimemazine) had high affinity for the muscarinic receptors (K1=5.0-38 nM). Another group of H1 -receptor antagonists (mepyramine, terfenadine, metapyrilen, azelastine, hydroxyzine and meclizine) had low affinity for the muscarinic receptors (K1=3, 600-30, 000 nM). Thus, a broad range of antimuscarinic potencies among the antihistamines was demonstrated. These results should provide helpful information with regard to the clinical and experimental use of antihistamines.

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