Relationship between anti-acetylcholine and anti-Tremorine activity in anti-parkinsonian and related drugs

Abstract

The anti-acetylcholine potency of a number of anti-Parkinsonism drugs and related phenothiazine compounds was determined using the isolated guinea-pig ileum. The antagonism was assessed by the difference between the pA(2) and pA(10) values and by log concentration-response curves for acetylcholine in presence and absence of the antagonists. All compounds except chlorpromazine showed some evidence of competitive antagonism to acetylcholine. The anti-tremor potency of the compounds was assessed from suppression of Tremorine-induced tremors in mice. There was a relation between anti-acetylcholine and anti-Tremorine potency among the anti-Parkinsonism drugs, but not among the phenothiazine compounds. Some implications of the findings are discussed in relation to the mode of action of anti-Parkinsonism drugs.