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, Volume 19, Issue 3–4, pp 164–168 | Cite as

Antagonism of histamine and leukotrienes by azelastine in isolated guinea pig ileum

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

Abstract

The effects of azelastine on histamine- and leukotriene C4 and D4 (LTC4, LTD4)-induced contractile responses in isolated guinea pig ileum were investigated. Following a 2-min contact with the ileum, azelastine produced competitive antagonism of histamine (pA2=8.24). Following a 15-min contact, azelastine at 2.5×10−9 M exerted competitive antagonism, but at higher concentrations (10, 40 and 160×10−9M) it not only shifted histamine concentration-effect curves to the right but also suppressed its maximum. Thus, azelastine exerts a dual (competitive/noncompetitive) antagonism of histamine depending upon the concentration and duration of contact. Azelastine and FPL 55712 (a known LT receptor antagonist) produced concentration-dependent antagonism of LTC4 and LTD4. Azelastine and compound FPL 55712 also exerted concentration-dependent reversal (relaxation) of pre-existing LTC4-induced contractions. In conclusion, the potent H1-histamine and leukotriene receptor blocking activities of azelastine may contribute to its antiasthmatic/antiallergic activities.

Keywords

Receptor Antagonist Histamine Receptor Blocking Contractile Response Blocking Activity 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Birkhäuser Verlag 1986

Authors and Affiliations

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

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