Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Formation of p-Hydroxycocaine from Cocaine by Hepatic Microsomes of Animals and Its Pharmacological Effects in Mice
Kazuhito WATANABEYoko HIDATamihide MATSUNAGAIkuo YAMAMOTOHidetoshi YOSHIMURA
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1993 Volume 16 Issue 10 Pages 1041-1043

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Abstract

The hepatic microsomal metabolism of cocaine and the pharmacological effects of some metabolites were studied in experimental animals. Hepatic microsomes from mice, rats and guinea pigs catalyzed the oxidation of cocaine to m- and p-hydroxycocaines. Only trace amounts of m-hydroxycocaine were detected in the extract of the incubation mixture with rabbit hepatic microsomes. The total amount of the two hydroxycocaines was less than 12% that of norcocaine which was the most predominant microsomal metabolite in all the animal species examined. The administration of p-hydroxycocaine (20 mg/kg i.p.) to mice significantly increased locomotor activity (total distance and number of rearing movements). The effect of p-hydroxycocaine was more active or comparable with that of cocaine, indicating that this metabolite is an active metabolite of cocaine.

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© The Pharmaceutical Society of Japan
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