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.
Baba
A
A
Department of Psychopharmacology, Tokyo Institute of Psychiatry, Japan.
Yamamoto
T
T
Yamamoto
H
H
Suzuki
T
T
Moroji
T
T
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D018492:Dopamine Antagonists / Q000494:pharmacology; D008297:Male; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013574:Synaptosomes / Q000378:metabolism; D014316:Tritium
D018492:Dopamine Antagonists; D014316:Tritium; C031107:4-phenyl-4-piperidinocyclohexanol; C012058:tenocyclidine; D010622:Phencyclidine; D004298:Dopamine