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实验性抗精神病药物4-[4-(对氯苯甲酰基)哌啶基]-4'-氟丁酰苯的基本代谢产物鉴定

Identification of basic metabolites of 4-[4-(p-chlo- robenzoyl)piperidino]-4'-fluorobutyrophenone, an experimental neuroleptic agent.

作者信息

Fusaro G A, Garteiz D A, Chan K Y, Leeson G A

出版信息

Drug Metab Dispos. 1976 Nov-Dec;4(6):562-7.

PMID:11978
Abstract

Two metabolites of 4-[4-(p-(chlorobenzoyl)piperidino]-4'-fluorobutyrophenone (RMI 9901) as well as unchanged drug, have been identified in the urine of rats following oral administration of the drug. Analysis of basic urine extracts by combined gas chromatography-mass spectrometry was employed for metabolite identification. N-dealkylation appears to be a major metabolic pathway and results in formation of 4-(p-chlorobenzoyl)piperidine (I). Subsequent oxidation of this metabolite results in the formation of 4-(p-chlorobenzoyl)-2-piperidone (II), and represents rather unusual metabolic pathway for compounds of this chemical class.

摘要

大鼠口服4-[4-(对氯苯甲酰基)哌啶基]-4'-氟丁酰苯(RMI 9901)后,在其尿液中已鉴定出该药物的两种代谢产物以及未变化的药物。采用气相色谱-质谱联用分析法对碱性尿液提取物进行分析以鉴定代谢产物。N-脱烷基化似乎是主要的代谢途径,会生成4-(对氯苯甲酰基)哌啶(I)。该代谢产物随后的氧化会生成4-(对氯苯甲酰基)-2-哌啶酮(II),这对于此类化学化合物而言是相当不寻常的代谢途径。

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