1-Allyl and 1-(3, 3-dimethylallyl) analogues of pethidine and its reversed ester

Author:

Casy A F1,Simmonds A B1,Staniforth D1

Affiliation:

1. Department of Pharmacy, Chelsea College of Science and Technology (University of London), London, S.W.3, England

Abstract

Abstract The preparation of some 1-allyl and 1-(3, 3-dimethylallyl)-4-phenylpiperidines related to pethidine and its reversed ester is described and the hot-plate activities in mice of these compounds reported. All six derivatives displayed morphine-like properties in mice, four being more potent (1·5–6 times) than morphine, but failed to act as analgesic antagonists in rats. The results are contrasted with the properties of similarly N-substituted fused-ring analgesics and differences discussed in terms of drug-receptor interaction modes.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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