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苯环利定及其N-乙胺类似物在大鼠体内的处置动力学。

The dispositional kinetics of phencyclidine and its N-ethylamine analogue in rats.

作者信息

Chakrabarti S, Law F C

出版信息

Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):383-8. doi: 10.1007/BF03188770.

Abstract

The uptake kinetics of [3H]-labelled phencyclidine (PCP) and N-ethyl-l-phenycyclohexylamine (PCE) in rats, measured in terms of decreases in the blood concentrations of the drugs after i.v. administration of a single 1.09 mumol dose, were not significantly different. Within a week of administration, the rats excreted about 93% of the [3H]-PCP and about 65% of [3H]-PCE via their urine and faeces; their urine contained nore [3H], mainly as metabolites of [3H]-PCP and of [3H]-PCE, than their faeces. Similarly, more [3H] remained in the tissues of rats treated with [3H]-PCE than in the tissues of [3H4-PCP-treated rats. The fact that PCE is metabolized and excreted more slowly than PCP may account for the higher psychotropic effects of PCE.

摘要

以静脉注射单次1.09微摩尔剂量后药物血药浓度的降低来衡量,大鼠体内[3H]标记的苯环己哌啶(PCP)和N-乙基-1-苯基环己胺(PCE)的摄取动力学无显著差异。给药后一周内,大鼠通过尿液和粪便排泄了约93%的[3H]-PCP和约65%的[3H]-PCE;它们尿液中含有的[3H]比粪便中更多,主要是[3H]-PCP和[3H]-PCE的代谢产物。同样,用[3H]-PCE处理的大鼠组织中残留的[3H]比用[3H]-PCP处理的大鼠组织中更多。PCE比PCP代谢和排泄更慢这一事实可能解释了PCE更高的精神效应。

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