A selective histamine H1 receptor antagonist
(R)-Cetirizine is the (R)-enantiomer of the histamine H1 receptor antagonist and second generation antihistamine cetirizine . (R)-Cetirizine binds to the H1 receptor with higher affinity than cetirizine (Kis = 3 and 6 nM, respectively) and is 25,000-100,000-fold selective for H1 receptors over muscarinic M1-M5 receptors. It decreases production of RANTES and eotaxin following antigen stimulation in mouse eosinophils in vitro in a concentration-dependent manner with a minimum effective concentration (MEC) of 0.05 µM. Intranasal administration of (R)-cetirizine (0.01-1%) dose-dependently decreases histamine-induced nasal rubbing and sneezing in mice. Formulations containing (R)-cetirizine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.
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