A muscarinic acetylcholine receptor antagonist
Procyclidine is an antagonist of muscarinic acetylcholine receptors (Kis = 4.47, 42.66, 7.24, 6.03, and 4.79 nM for M1-5 receptors, respectively).1 It increases fine motor activity counts (ED50 = 1.74 mg/kg) without affecting ambulatory activity in rats in a home-cage activity test.2 Formulations containing procyclidine have been used in the treatment of parkinsonism and extrapyramidal dysfunction.
1.Lazareno, S., Buckley, N.J., and Roberts, F.F.Characterization of muscarinic M4 binding sites in rabbit lung, chicken heart, and NG108-15 cellMol. Pharmacol.38(6)805-815(1990) 2.Sipos, M.L., Burchnell, V., and Galbicka, G.Dose-response curves and time-course effects of selected anticholinergics on locomotor activity in ratsPsychopharmacology147(3)250-256(1999)
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Animal experiment: |
Rats[1] Adult Sprague-Dawley female rats (weight 300-330 g) are used. Procyclidine given systemically causes a transient increase in locomotor activity (mainly non-ambulatory fine movements) in adult rats. Locomotor activity data (ambulations, fine movements) are evaluated using a two-way ANOVA to test whether co-administration of clonidine (0.025 mg/kg) with various doses of Procyclidine (10, 25, 50 and 75 mg/kg) altered the activity levels compared to the same doses of Procyclidine administered alone. A one-way ANOVA and subsequent comparisons are also conducted to establish whether the activity levels for each treatment group are different from saline controls. |
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参考文献: [1]. Jevtovic-Todorovic V, et al. Anti-parkinsonian agents procyclidine and ethopropazine alleviate thermal hyperalgesia in neuropathic rats. Neuropharmacology. 2003 May;44(6):739-48. |
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