醋酸艾塞那肽在大鼠体内的代谢分布(英文)  

Tissue distribution of exendin-4 in rats

作　　者：艾国[1] 陈知航[1] 单成启[1] 车津晶[1] 候禹男[1] 程远国[1] 

机构地区：[1]军事医学科学院微生物流行病研究所药物代谢动力学实验室,北京100071

出　　处：《中国药理学与毒理学杂志》2008年第2期95-101,共7页Chinese Journal of Pharmacology and Toxicology

基　　金：国家高技术研究发展计划资助项目(2003AA2Z347B)~~

摘　　要：目的研究醋酸艾塞那肽(exendin-4)在大鼠体内的组织分布。方法Iodo-GenTM法制备[125I]exendin-4,大鼠皮下注射[125I]exendin-4后,分别测定血浆或组织中的总放射性含量和酸沉淀放射性含量。结果[125I]exendin-4的酸沉淀放射性分布从高到低的顺序为肾脏>肺>膀胱>胰腺>肠>血浆>肾上腺>空肠>淋巴结>肝>脾>心脏>骨髓>胸腺>睾丸>脑>肌肉>脂肪。结论[125I]ex-endin-4的分布快速而广泛,其中以肾脏中最高,而在脑组织只发现微量的[125I]exendin-4。AIM To investigate the tissue distribution of exendin-4 after administration in healthy rats. METHODS Exendin-4 was radioiodinated by the Iodo-Gen^TM method. Tissue distribution of [ ^125I]exendin-4 was inves- tigated after sc administration of [^125I ] exendin-4 at 3μg.kg.-1 in rats. Both total radioactivity and trichloroacetic acid （TCA） precipitated radioactivity were used to calculate the levels of [^125I ] exendin-4 in rats plasma and tissue samples after sc administration. RESULTS The tissue distribution of [ ^125I ] exendin-4 after sc injection showed substantial disposition in kidneys, lungs, bladder and pancreas. The rank order of normalized tissue distribution was kidneys 〉 lungs 〉 bladder 〉 pancreas 〉 intestine 〉 plasma 〉 adrenals 〉 jejunum 〉 lymph 〉 liver 〉 spleen 〉 heart 〉 marrow 〉 thymus 〉 testicles 〉 brain 〉 muscle 〉adipose. CONCLUSION [^125I]Exendin-4 un- derwent a rapid and wide distribution in the tissues throughout the whole body within the time course examined. TCA precipitated radioactivity in kidneys was the highest, however, only trace amounts of [ ^125I ] exendin-4 was detected in the brain.

关 键 词：醋酸艾塞那肽 组织分布 药代动力学 

分 类 号：R96[医药卫生—药理学]