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Trihexyphenidyl is an antagonist of M1 muscarinic acetylcholine receptors.1 It binds to rat M1 receptors in cerebral cortex selectively over rat M2 receptors in heart tissue (IC50s = 3.7 and 31 nM, respectively). Trihexyphenidyl inhibits contractions induced by acetylcholine (Item No. 23829) in guinea pig ileum (IC50 = 22 nM).2 It also inhibits oxotremorine-induced tremors and physostigmine-induced mortality in mice (ED50s = 2 and 3.6 mg/kg, respectively). Trihexyphenidyl (20 mg/kg) improves abnormal movement in a mouse model of L-3,4-dihydroxyphenylalanine (L-DOPA) responsive dystonia (DRD) that expresses mutant tyrosine hydroxylase (TH).3 Formulations containing trihexyphenidyl have been used in the symptomatic treatment of Parkinson's disease.
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1. Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br. J. Pharmacol. 89(1), 83-90 (1986).
2. Peripheral and central muscarinic receptor affinity of psychotropic drugs. Naunyn. Schmiedebergs. Arch. Pharmacol. 301(1), 5-9 (1977).
3. A new knock-