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Tripelennamine is a histamine H1 receptor antagonist (Ki = 7.4 nM).1 It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs; Ki = 1,300 nM). Tripelennamine also selectively inhibits histamine- over acetylcholine-induced contractions in isolated guinea pig ileum segments (EC50s = 14 and 7,800 nM, respectively), as well as serotonin-induced contractions in isolated rat uterus (EC50 = 14,000 nM).2 It protects against histamine-induced lethality and dyspnea in guinea pigs with half-maximal protective dose (PD50) values of 2.74 and 1.2 mg/kg, respectively. Formulations containing tripelennamine have been used as antihistamines in veterinary medicine.
WARNING This product is not for human or veterinary use.
1. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptor-
2. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions 4(4), 264-270 (1974).