THE METABOLISM OF PHENCYCLIDINE BY RABBIT LIVER PREPARATIONS

  • 1 January 1981
    • journal article
    • research article
    • Vol. 9  (3) , 274-278
Abstract
The in vitro metabolism of phenycyclidine by rabbit liver 9000 g supernatant fraction produces primarily 3 known hydroxylated metabolites.sbd.namely, 4-phenyl-4-piperidinocyclohexanol, 4-(4''-hydroxypiperidino)-4-phenylcyclohexanol and 1-(1-phenylcyclohexyl)-4-hydroxypiperidine.sbd.plus a new metabolite formed by oxidative scission of the piperidine ring yielding an aminoalcohol, and much smaller amounts of 5 unidentified metabolites. Incubation with 50% deuterium-labeled PCP indicates that these compounds are metabolites by monitoring the resulting doublets found in their mass spectra. The time, cofactor and protein-dependent formation of the compounds confirms that they are metabolites. DPEA-(2,4-dichloro-6-phenylphenoxyethylamine) inhibits the production of the 4 quantitated metabolites with maximal I50 [median inhibitory concentration] values of .apprx. 50 .mu.M, implying the involvement of cytochrome P-450 in these reactions.

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