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Description: Astemizole (also knwo as R-43512) is a novel, potent and second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, it acts as a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has anticholinergic and antipruritic effects. Astemizole competitively binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus caused by histamine. Astemizole is structurally similar to terfenadine and haloperidol.
References: Drugs. 1984 Jul; 28(1):38-61.
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