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正电子发射断层扫描期间血浆[18F]-6-氟多巴的测定:卡比多巴治疗受试者的消除和代谢

Determination of plasma [18F]-6-fluorodopa during positron emission tomography: elimination and metabolism in carbidopa treated subjects.

作者信息

Boyes B E, Cumming P, Martin W R, McGeer E G

出版信息

Life Sci. 1986 Dec 8;39(23):2243-52. doi: 10.1016/0024-3205(86)90403-0.

Abstract

An investigation of the metabolism of [18F]-6-fluorodopa (FDOPA) given to carbidopa treated subjects for scanning by positron emission tomography (PET) has been carried out by analysis of plasma. Reverse phase ion pair HPLC and alumina extraction were employed to fractionate and identify the [18F]-labelled compounds of plasma over a two hour period. During this time, the plasma levels of both total 18F and FDOPA decreased as a bi-exponential function of time. The rates of 18F, but not FDOPA, elimination were observed to decrease with age. In addition to FDOPA, only one other major peak of radioactivity was resolved by HPLC. Identification of this compound as the O-methylated derivative of FDOPA (MeFDOPA) is based on its shared HPLC elution time with in vitro synthesized O-[methyl-14C]-FDOPA. The ratio of the concentration of MeFDOPA to FDOPA (MeFDOPA/FDOPA) in plasma increased linearly with time, and the slope of this linear relationship decreased with the age of the individual.

摘要

通过对血浆的分析,对给予卡比多巴治疗的受试者用于正电子发射断层扫描(PET)的[18F]-6-氟多巴(FDOPA)的代谢情况进行了研究。采用反相离子对高效液相色谱法(HPLC)和氧化铝萃取法,在两小时内对血浆中的[18F]标记化合物进行分离和鉴定。在此期间,总18F和FDOPA的血浆水平均呈双指数时间函数下降。观察到18F的消除速率随年龄增长而降低,但FDOPA的消除速率不受年龄影响。除FDOPA外,HPLC仅分离出另一个主要放射性峰。将该化合物鉴定为FDOPA的O-甲基化衍生物(MeFDOPA),是基于其与体外合成的O-[甲基-14C]-FDOPA具有相同的HPLC洗脱时间。血浆中MeFDOPA与FDOPA的浓度比(MeFDOPA/FDOPA)随时间呈线性增加,且该线性关系的斜率随个体年龄增长而降低。

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