H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects.

  title={H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects.},
  author={Rob Leurs and M K Church and Maurizio Taglialatela},
  journal={Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology},
  volume={32 4},
This review addresses novel concepts of histamine H1-receptor function and attempts to relate them to the anti-inflammatory effects of H1-antihistamines. Furthermore, the molecular mechanisms underlying the cardiotoxic effects of H1-antihistamines are discussed. H1-receptors are G-protein-coupled-receptors (GPCRs), the inactive and active conformations of which coexist in equilibrium. The degree receptor activation in the absence of histamine is its 'constitutive activity'. In this two-state… CONTINUE READING
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