In vitro metabolism of procyclidine in the rat

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Abstract
Procyclidine, l-cyclohexyl-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, was incubated with the 9000g supernatant fraction of rat liver homogenates, fortified with a NADPH generating system. Three major metabolites were isolated from the incubation mixture. They were identified as 1-(cis-4-hydroxycycloherxyl)-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, 1-(trans-4-hydroxycyclohexyl)-1-phenyl-3-(1-pyrrolidinyl)-1-propanol, and (1R* 3R*, 7S(R?)*)-1-(trans-3-hydroxycyclohexyl)-1-phenyl-3-(1-pyrrolidinyl)-1-propanol. The latter has not been detected previsiouly in rat urine and probably represents an intermediate metabolite. Send reprint request to: G. Paeme, Vrije Universiteit Brussel, Farmaceutisch Instituut, Eenheid Farmacognosie, Fytochemie en Toxicologie, Laarbeeklaan, 103, B-1090 Brussel, Belgium.