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Sites of Action of some Partial Agonists on the Isolated Guinea-pig Ileum

Abstract

IT is well known that if in a homologous series of drugs a special group is changed by heavier ones, they gradually change from agonists through partial agonists into competitive antagonists1. It has been reported that isoamyl acetate, its analogues2 and pilocarpine3, some of which are partial agonists, contract the isolated guinea-pig ileum through the liberation of acetylcholine on the one hand, and antagonize the action of released acetylcholine on the other hand, when they combine with the acetylcholine receptor. The sites of action of partial agonists, however, have never been studied precisely, and so we have investigated the effects of cooling, cocaine, morphine and hexa-methonium on the actions of two series of drugs which are esters of choline and dimethylaminoethanol.

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TAKAGI, K., TAKAYANAGI, I., TAGA, F. et al. Sites of Action of some Partial Agonists on the Isolated Guinea-pig Ileum. Nature 217, 573–574 (1968). https://doi.org/10.1038/217573a0

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