title: Azelastine inhibits IgE-mediated human basophil histamine release.
abstract: To examine the mechanism potentially contributing to therapeutic efficacy of azelastine in allergic rhinitis and asthma, we studied the effect of azelastine on stimulated histamine release from basophils prepared as a mixed leukocyte suspension from human blood. Azelastine was found to significantly inhibit anti-IgE-stimulated basophil histamine release. Time-course experiments indicated that the inhibitory effect of azelastine was immediate and that preincubation of basophils in azelastine was not necessary. In dose-response experiments with azelastine, 1 to 100 mumol/L, significant inhibition of histamine release was consistently observed in azelastine concentrations greater than or equal to 10 mumol/L. This inhibition was dose dependent (r = 0.96; p less than 0.001) with maximal mean inhibition of 91 +/- 8% at 100 mumol/L of azelastine.
authors: Department of Internal Medicine, Veterans Administration Medical Center, Iowa City, Iowa.
authors: M M
authors: MM
authors: Little
authors: T B
authors: TB
authors: Casale
mesh_terms: D001491:Basophils / Q000187:drug effects* / Q000378:metabolism; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D007073:Immunoglobulin E / Q000502:physiology; D066298:In Vitro Techniques; D010793:Phthalazines / Q000494:pharmacology*; D011724:Pyridazines / Q000494:pharmacology*
chemical_list: D010793:Phthalazines; D011724:Pyridazines; D007073:Immunoglobulin E; C020976:azelastine