On the Pharmacological Effect of Dimethylpethidine and its Alkylsulfone Substituentes

Abstract

Analgesic, sedative, and anticonvulsant activities and toxicity of ethyl 1-methyl-4- (3′, 4′-dimethylphenyl) piperidine-4-carboxylate (Dimethylpethidine) and 1-methyl-4-(3′, 4′, -dimethylphenyl) piperidyl-4-methyl (or ethyl) sulfone were compared with those of Pethidine. Analgesic action of Dimethylpethidine was slightly weaker than that of Pethidine but the anticonvulsant action was about equal, analgesic action was stronger, and toxicity was weaker, LD₅₀ being 0.29mg./g. mouse by subcutaneous injection. The compound obtained by the substitution of ethoxycarbonyl group in Dimethylpethidine with methyl (or ethyl) sulfone possessed weaker analgesic and anticonvulsant action than those of Pethidine, with equal or stronger analgesic action, and weaker toxicity.