大鼠经口暴露后驱虫剂N,N-二乙基苯乙酰胺的分布与代谢

Distribution and metabolism of insect repellant N,N-diethylphenylacetamide on oral exposure in rats.

作者信息

Rao S S, Jaiswal D K, Ramachandran P K

机构信息

Biochemistry Division, Defence Research and Development Establishment, Gwalior, India.

出版信息

Toxicol Lett. 1991 Mar;55(3):243-8. doi: 10.1016/0378-4274(91)90003-o.

DOI:10.1016/0378-4274(91)90003-o

PMID:2003266

Abstract

Oral toxicity, distribution and metabolism of a new multi-insect repellant, N,N-diethylphenylacetamide (DEPA) was studied in rats. On administration of DEPA (851 mg/kg body wt.) labelled with 14C blood, liver, stomach and stomach contents had 2.65, 3.97, 12.07 and greater than 50.66% radioactivity, respectively, after 20 min. Gas chromatographic analysis showed presence of both DEPA and its metabolite N-ethylphenylacetamide (EPA) in blood, liver, kidneys and lungs while only DEPA was present in stomach and stomach contents. EPA, phenylacetamide and conjugated phenylacetic acid were excreted along with unmetabolized parent compound in urine of rats when a low oral dose of DEPA (70 mg/kg body wt.) was administered. Activities of erythrocyte cholinesterase and carbonic anhydrase did not change significantly upon acute oral exposure to DEPA.

摘要

在大鼠中研究了一种新型多昆虫驱避剂N,N-二乙基苯乙酰胺（DEPA）的口服毒性、分布和代谢。给予标记有14C的DEPA（851毫克/千克体重）后20分钟，血液、肝脏、胃和胃内容物中的放射性分别为2.65%、3.97%、12.07%和大于50.66%。气相色谱分析表明，血液、肝脏、肾脏和肺中同时存在DEPA及其代谢物N-乙基苯乙酰胺（EPA），而胃和胃内容物中仅存在DEPA。当给予低口服剂量的DEPA（70毫克/千克体重）时，EPA、苯乙酰胺和共轭苯乙酸与未代谢的母体化合物一起从大鼠尿液中排出。急性口服DEPA后，红细胞胆碱酯酶和碳酸酐酶的活性没有显著变化。