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大鼠体内[14C]去甲异克卓明的代谢情况

[14C]normacromerine fate in the rat.

作者信息

Ferguson P W, Keller W J, Risinger F O

出版信息

J Pharm Sci. 1984 May;73(5):692-3. doi: 10.1002/jps.2600730527.

DOI:10.1002/jps.2600730527
PMID:6737246
Abstract

The biological fate of [14C] normacromerine , a dimethoxylated phenethylamine derivative with putative hallucinogenic properties, was evaluated in male Sprague-Dawley rats at 100 mg/kg po. Urine was the primary elimination route accounting for 50% of administered carbon-14 after 24 h. Of this urine radioactivity, normacromerine comprised 30% at 8 h decreasing to nondetectable levels at 24h. Carbon-14 in feces represented less than 10% of the administered dose at 24 h, and 14CO2 expiration was not detected. Studies of normacromerine fate in comparison with previously studied phenethylamines may enhance evaluation of hallucinogenic potential of normacromerine .

摘要

对具有假定致幻特性的二甲氧基苯乙胺衍生物[14C]去甲大麦芽碱,以100mg/kg的剂量经口给予雄性斯普拉格-道利大鼠,评估其生物学转归。尿液是主要的排泄途径,24小时后占给予碳-14的50%。在该尿液放射性中,去甲大麦芽碱在8小时时占30%,至24小时降至无法检测的水平。粪便中的碳-14在24小时时占给予剂量的不到10%,且未检测到14CO2呼出。将去甲大麦芽碱的转归研究与之前研究的苯乙胺进行比较,可能会加强对去甲大麦芽碱致幻潜力的评估。

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