EFFECTS OF THE MAJOR METABOLITE OF PHENCYCLIDINE, THE TRANS ISOMER OF 4-PHENYL-4-(1-PIPERIDINYL)CYCLOHEXANOL, ON [H-3] N-(1-[2-THIENYL]CYCLOHEXYL)-3,4-PIPERIDINE ([H-3]TCP) BINDING AND [H-3] DOPAMINE UPTAKE IN THE RAT-BRAIN

The major metabolite of phencyclidine (PCP), the trans isomer of 4-phenyl-4-(1-piperidinyl)cyclohexanol [(trans)4-PPC], inhibited [H-3]N-(1-(2-thienyl)cyclohexyl)-3,4-piperidine ([H-3]TCP) binding to well-washed rat cortical membranes with much less activity than PCP itself. In contrast, it inhibited [H-3]dopamine ([H-3]DA) uptake in rat striatal synaptosomes to a similar extent as PCP. Considering our previous observations that intraperitoneally administered (trans)-4-PPC elicits dose-related increases in locomotor activity and rearing in mice, (trans)4-PPC as well as PCP may be involved in psychotomimetic effects of PCP due to its inhibitory effect on DA uptake.