小动物正电子发射计算机断层扫描技术在药动学研究中的应用

Micro-PET imaging used in pharmacokinetic study

作为一种活体生化显像技术以及核医学领域最先进的临床检查影像技术的延伸,小动物正电子发射计算机断层扫描(Micro-PET)利用[11C],[13N],[15O],[18F]等发射正电子的短半衰期核素标记的各种药物或内源性化合物或生化标志物,通过显像,可以在体内无创伤、定量、动态地观察机体的生理、生化变化,观察标记物的体内动力学过程,揭示药物转运、分布以及药物相互作用、药效靶点甚至产生毒性的分子机制。本文就Micro-PET的基本原理及其在药动学研究中的应用进展作阐述。

As one of the most developed functional imaging techniques in nuclear medicine and imaging techniques in visualization of living animals, micro-PET can visually, non-invasively, dynamically and quantitative- ly image the kinetics of radiotracers in vivo, and provide mechanic insight into drug transport, drug distribution, drug-drug interaction, site of drug action and toxicity. Radionuclides used in micro-PET scanning are typical iso- topes with short half-lives such as [^11C] （ -20 min）, [^13N] （ -10 min）, [^15O] （ -2 min）, or [^18F] （ -110 min）. They are incorporated either into compounds normally used by the body such as glucose （or glucose analogues） , water or ammonia, or into molecules that bind to receptors or other sites of drug action, or into drugs. In this paper, we summarized the principals of micro-PET imaging and its application in pharmacokinetic research and new drug development.