Boggan W O, Stringer A J, Faught K, Middaugh L D
Pharmacol Biochem Behav. 1987 Apr;26(4):847-9. doi: 10.1016/0091-3057(87)90620-4.
The purpose of these investigations was to determine if phencyclidine (PCP) and/or two of its major monohydroxy metabolites [1-(1-phenylcyclohexyl)4-hydroxy piperidine (4-OH-pip PCP) and 1-(1-phenyl-4-hydroxycyclohexyl) piperidine (4-OH-cyclo PCP)] influence 3H quinuclidinyl benzilate (QNB) binding in rat brain after in vivo administration. PCP and 4-OH-pip PCP but not 4-OH-cyclo PCP enhanced QNB binding. The effect was blocked by atropine. Since the dose of 4-OH-pip PCP necessary to alter QNB binding in rat brain is substantially higher than that required for PCP, this metabolite probably does not play a major role in the PCP effect on QNB binding in rat brain.
这些研究的目的是确定在体内给药后,苯环己哌啶(PCP)及其两种主要的单羟基代谢产物[1-(1-苯基环己基)-4-羟基哌啶(4-OH-pip PCP)和1-(1-苯基-4-羟基环己基)哌啶(4-OH-cyclo PCP)]是否会影响大鼠脑中3H-东莨菪碱(QNB)的结合。PCP和4-OH-pip PCP可增强QNB结合,但4-OH-cyclo PCP无此作用。该作用可被阿托品阻断。由于改变大鼠脑中QNB结合所需的4-OH-pip PCP剂量远高于PCP所需剂量,因此该代谢产物可能在PCP对大鼠脑中QNB结合的作用中不起主要作用。