Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes.

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Mita H, Shida T

Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes.

Arzneimittelforschung. 1995 Jan;45(1):36-40.

PubMed ID

7893266 [ View in PubMed

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Abstract

The effects of three histamine H1 receptor antagonists, epinastine (CAS 80012-43-7, WAL-801 CL), ketotifen (CAS 34580-13-7) and oxatomide (CAS 60607-34-3), on mediator release have been studied in human peripheral leukocytes. When leukocytes from asthmatic patients sensitive to mite were stimulated with the allergen, epinastine inhibited histamine release with a concentration required for 50% inhibition (IC50) of 3 x 10(-5) mol/l and leukotriene C4 generation. On the other hand, ketotifen or oxatomide showed little inhibiting effect on histamine release elicited with the allergen. When the cells were stimulated with calcium ionophore A23187, epinastine failed to inhibit histamine release and leukotriene C4 generation. Oxatomide caused a concentration related inhibition of calcium ionophore-induced histamine release with the IC50 value of 5 x 10(-5) mol/l. Ketotifen or oxatomide also showed an inhibition of leukotriene C4 generation induced by calcium ionophore in a dose-dependent manner and the IC50 value was 6 x 10(-6) mol/l for oxatomide and 8 x 10(-5) mol/l for ketotifen, suggesting that oxatomide is a more potent inhibitor of leukotriene C4 generation than ketotifen. These results indicate that epinastine inhibits IgE-mediated histamine release and LTC4 generation, and oxatomide has a capacity to inhibit calcium ionophore-induced mediator release from human leukocytes. Additionally, when platelet activating factor was quantitated by radioimmunoassay in the supernatant and the cell pellet after ionophore stimulation, epinastine inhibited the formation and the secretion in a dose-dependent manner.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Ketotifen	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details