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[口服水合氯醛后人体中神经毒素1-三氯甲基-1,2,4,5-四氢-β-咔啉(TaClo)的血浆水平]

[The plasma level of the neurotoxin 1-trichloromethyl-1,2,4,5-tetrahydro-beta-carboline (TaClo) in man after oral administration of chloral hydrate].

作者信息

Leuschner J, Beuscher N, Zimmermann T, Schürer M, Schulz H U, Jeromin J, Ritter H

机构信息

LPT Laboratory of Pharmacology and Toxicology, Hamburg.

出版信息

Arzneimittelforschung. 1998 Jan;48(1):1-5.

PMID:9522023
Abstract

Chloral hydrate (CAS 302-17-0) is a widely used hypnotic and sedative agent. It was recently reported in the literature that a neurotoxin, TaClo (1-trichloromethyl-1,2,3,4-tetrahydro-beta-carboline), may be formed in vitro from tryptamine (Ta) and chloral (Clo). Intraperitoneal administration of TaClo led to parkinson-like symptoms in the rat. Hence, the plasma levels of TaClo were determined at various time-points in 18 healthy volunteers in two periods each during a bioavailability study of several chloral hydrate preparations. The limit of quantitation for TaClo was 5 ng/ml. No TaClo could be determined in the plasma of the various volunteers following administration of human therapeutic doses of chloral hydrate. Hence, it is unlikely that TaClo will be formed in man after application of therapeutic doses of chloral hydrate to patients.

摘要

水合氯醛(CAS 302-17-0)是一种广泛使用的催眠和镇静剂。最近文献报道,一种神经毒素TaClo(1-三氯甲基-1,2,3,4-四氢-β-咔啉)可能在体外由色胺(Ta)和水合氯醛(Clo)形成。腹腔注射TaClo会导致大鼠出现帕金森样症状。因此,在几种水合氯醛制剂的生物利用度研究中,在两个时间段对18名健康志愿者在不同时间点测定了TaClo的血浆水平。TaClo的定量限为5 ng/ml。在给予人类治疗剂量的水合氯醛后,各志愿者的血浆中均未检测到TaClo。因此,在对患者应用治疗剂量的水合氯醛后,人体不太可能形成TaClo。

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