Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole

6533b7cffe1ef96bd1258566

RESEARCH PRODUCT

Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole

L. Estañ Francisco J. Morales-olivas Inocencia Martínez-mir Elena Rubio

subject

medicine.medical_specialty Duodenum medicine.drug_class medicine.medical_treatment Guinea Pigs Pharmaceutical Science In Vitro Techniques Biology Parasympatholytic chemistry.chemical_compound Phenothiazines Internal medicine medicine Anticholinergic Animals Potency Mequitazine Pharmacology Parasympatholytics Muscle Smooth Rats Inbred Strains Acetylcholine Rats Clemizole Schild regression Endocrinology chemistry Histamine H1 Antagonists Benzimidazoles Antihistamine Histamine Histamine Muscle Contraction medicine.drug

description

Abstract The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plot were 9.95 ± 0.44 for mequitazine and 10.54 ± 0.44 for clemizole. Mequitazine at 10−7 M produced a parallel shift of the dose-response curve to acetylcholine in the rat duodenum, clemizole and the lower doses of mequitazine failed to modify the effect of acetylcholine. The potency of mequitazine and clemizole as H1-histamine blockers is similar, but only mequitazine at highest concentration used showed anticholinergic activity.

year	journal	country	edition	language
1988-09-01	Journal of Pharmacy and Pharmacology

https://doi.org/10.1111/j.2042-7158.1988.tb05331.x

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