増感作用の薬理学的研究(第1報)Cocaineのモルモット摘出精管増感作用の用量反応相関

概要

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In order to clarify the mechanism of the so-called "nonspecific supersensitization" induced by cocaine, effect of cocaine on dose-response curves of various agonists was examined with isolated vas deferens of a guinea pig. Cocaine increased the sensitivity but did not change the maximum response of vas deferens to norepinephrine, epinephrine, and acetylcholine. Increase in the degree of supersensitivity to acetylcholine was dose-dependent up to 3×10^<-5>M, while that to norepinephrine and epinephrine decreased at the concentration of 3×10^<-5>M of cocaine. Cocaine did not change the affinity of norepinephrine and acetylcholine receptors to phentolamine and atropine, respectively. Higher concentration of cocaine was required to induce rhythmic contraction and supersensitivity to acetylcholine of vas deferens from older guinea pigs. Cocaine induced slight increases in the sensitivity and maximum response of vas deferens to histamine. These results suggest that cocaine-induced supersensitivity to acetylcholine is elicited through post-junctional beyond-receptor mechanism and does not contribute to the potentiation of contractile response to catecholamines and histamine by cocaine.
社団法人日本薬学会の論文
1975-09-25