Biomolecules & Therapeutics
- Volume 9 Issue 4
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- Pages.282-284
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- 2001
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- 1976-9148(pISSN)
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- 2005-4483(eISSN)
Comparison of the Antihistaminic Activity Between Cetirizine Enantiomers
- Park-Choo, Hae-Young (School of pharmacy, Ewha Womans University) ;
- Choi, Sun-Ok (Division of Biopharmaceutics and Clinical Pharmacology, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug) ;
- Lee, Seok-Ho (Department of Biologica Evaluation, Korea Food and Drug Administration)
- Published : 2001.12.01
Abstract
The antiallergic drug, cetirizine, inhibits the histamine release from a rat basophilic leukemia (RBL-2H3) cell line, which is frequently used as a mast cell model. By investigating inhibitory activities of (+)- and (-)-cetirizine in RBL-2H3 cells on the histamine release, we aimed to evaluate the effect of their structual characteristics on the antihistamine activity. The study on RBL-2H3 cell has clearly demonstrated that the (-)-cetirizine is significantly more potent than the (+)- or the racemic cetirizine, although there was no difference in pharmacokinetics between (+)- and (-)-cetirizine in rats.