Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics

European Journal of Pharmacology
B ChristopheR Massingham

Abstract

We characterised histamine H(1) receptor antagonism by cetirizine and its enantiomers on isolated guinea pig ileum and trachea. Competitive or mixed (competitive and apparent noncompetitive) antagonism profiles were observed. The order of potency was: chlorpheniramine> or =mepyramine>levocetirizine>cetirizine> or =terfenadine>loratadine>dextrocetirizine. The inhibitory effects of cetirizine, levocetirizine, terfenadine and loratadine were slowly reversible compared to those of dextrocetirizine or mepyramine. Cetirizine and its enantiomers were inactive on L-type Ca(2+) channels. Reduction of the histamine H(1) receptor reserve by dibenamine in the ileum (100-fold higher than in the trachea) showed a gradual change from the competitive profile of dextrocetirizine and mepyramine to a mixed profile. The present results show that cetirizine and levocetirizine are selective competitive but slowly reversible histamine H(1) receptor antagonists. Their mixed antagonism profile observed in the trachea can be explained by the small receptor reserve present in this tissue compared to the ileum and their very slow dissociation rate from the histamine H(1) receptor.

References

Jul 1, 1991·The Journal of Allergy and Clinical Immunology·C AdvenierC De Vos
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Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

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Citations

Jan 4, 2006·European Journal of Pharmacology·Michel Gillard, Pierre Chatelain
Jul 17, 2013·Immunopharmacology and Immunotoxicology·Chie Kitayama-SugiyamaChiaki Kamei
Jul 30, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Reggie BosmaHenry F Vischer
May 20, 2005·World Journal of Gastroenterology : WJG·Hua Xie, Shao-Heng He

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