Mousa S A, Williams S J, Sands H
J Nucl Med. 1987 Aug;28(8):1351-7.
A variety of laboratory procedures can be used to define the chemistry and pharmacokinetics of myocardial cationic imaging agents. These methods are utilized to define the in vivo chemistry of cationic heart agents, in order to understand the kinetics and mechanisms of: tissue and cellular transport, subcellular distribution, and intracellular localization. Transport across cell membranes can be active, passive or facilitated. Studies performed in erythrocytes, heart cells, slices and isolated perfused hearts using methods for separation of metabolites have shown a high degree of myocardial specificity for [99mTc]hexakis alkyl isonitrile by an uptake mechanism different from 201Tl. These studies demonstrate the importance of in vivo chemistry and pharmacokinetics in the development of new radiopharmaceuticals.
多种实验室程序可用于确定心肌阳离子显像剂的化学性质和药代动力学。这些方法用于定义阳离子心脏显像剂的体内化学性质,以便了解组织和细胞转运、亚细胞分布及细胞内定位的动力学和机制。跨细胞膜的转运可以是主动的、被动的或易化的。利用代谢物分离方法在红细胞、心脏细胞、切片和离体灌注心脏中进行的研究表明,[99mTc]六烷基异腈对心肌具有高度特异性,其摄取机制不同于201Tl。这些研究证明了体内化学性质和药代动力学在新型放射性药物开发中的重要性。