Effects of the major metabolite of phencyclidine, the trans isomer of 4-phenyl-4-(1-piperidinyl)cyclohexanol, on [3H]N-(1-[2-thienyl] cyclohexyl)-3,4-piperidine ([3H]TCP) binding and [3H]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 [3H]N-(1-(2-thienyl)cyclohexyl)-3,4-piperidine ([3H]TCP) binding to well-washed rat cortical membranes with much less activity than PCP itself. In contrast, it inhibited [3H]dopamine ([3H]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.