Effect of Azelastine on Leukotriene Synthesis in Murine Peritoneal Cells and on Thromboxane Synthesis in Human Platelets
- 1 January 1989
- journal article
- research article
- Published by S. Karger AG in International Archives of Allergy and Immunology
- Vol. 90 (3) , 285-290
- https://doi.org/10.1159/000235039
Abstract
Azelastine, a newly synthesized antiallergic agent, strikingly inhibited the production of leukotriene B4 and C4 (LTB4 and LTC4) in murine peritoneal cells which had been stimulated by calcium ionophore A23187. The 50% inhibitory concentrations (IC50) of the agent were approximately 1.0 × 10––5M. In addition, azelastine significantly inhibited also 5-lipoxygenase activity in peritoneal cells with an IC50 of 1.0 × 10––5M, but not on LTC4 synthetase, LTA4 hydrolase or phospholipase A2 activity. Furthermore, azelastine showed little effect on either 12-lipoxygenase activity or thromboxane synthesis in human platelets. These results suggest that at least the drug’s antiallergic effects can be attributed to its inhibiting action of 5-lipoxygenase in regard to arachidonate metabolism.Keywords
This publication has 0 references indexed in Scilit: