Agents and Actions

, Volume 16, Issue 5, pp 318–322

Inhibition of IgE-mediated allergic histamine release from rat peritoneal mast cells by azelastine and selected antiallergic drugs

  • N. Chand
  • J. Pillar
  • W. Diamantis
  • R. D. Sofia
Histamine and Kinins

DOI: 10.1007/BF01982866

Cite this article as:
Chand, N., Pillar, J., Diamantis, W. et al. Agents and Actions (1985) 16: 318. doi:10.1007/BF01982866

Abstract

The ability of azelastine to inhibit IgE-mediated allergic histamine release from the peritoneal mast cells of actively sensitized rats was investigated and compared with selected antiallergic agents. Azelastine added simultaneously with the allergic stimuli (ovalbumin, OA, 10 μg/ml + phosphatidylserine, PS, 10 μg/ml) or preincubated with cells for 10 min prior to antigen challenge produced similar concentration-dependent inhibition of allergic histamine release. The IC50sM) following 10-min preincubation were as follows: azelastine = 4.8; astemizole = 86.3; ketotifen = 112.2; diphenhydramine = 133 and theophylline = 2040.3. At IC50 level azelastine was about 18, 23, 28 and 425 times as effective as astemizole, ketotifen (newer histamine H1-receptor antagonists), diphenhydramine (a traditional H1-receptor antagonist), and theophylline (a phosphodiesterase inhibitor), respectively. Sodium cromoglycate in a concentration range or 1–1000 μM (0 or 10-min preincubation) failed to exert any inhibitory effect. These data showed that among six drugs tested azelastine is the most potent inhibitor of allergic histamine release from rat peritoneal mast cells.

Copyright information

© Birkhäuser Verlag 1985

Authors and Affiliations

  • N. Chand
    • 1
  • J. Pillar
    • 1
  • W. Diamantis
    • 1
  • R. D. Sofia
    • 1
  1. 1.Department of Pharmacology, Wallace LaboratoriesDivision of Carter-Wallace, Inc.CranburyUSA