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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


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.


Receptor Antagonist Histamine Receptor Blocking Contractile Response Blocking Activity 


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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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