Jacobson G B, Watanabe Y, Valind S, Kuratsune H, Långström B
Uppsala University Pet Centre, Sweden.
Nucl Med Biol. 1997 Jul;24(5):471-8. doi: 10.1016/s0969-8051(97)00015-2.
The syntheses of L-carnitine, O-acetyl CoA, and O-acetyl-L-carnitine labelled with 11C at the 1- or 2-position of the acetyl group or the N-methyl position of carnitine, using the enzymes acetyl CoA synthetase and carnitine acetyltransferase, are described. With a total synthesis time of 45 min, O-[1-11C]acetyl CoA and O-[2[11C]acetyl CoA was obtained in 60-70% decay-corrected radiochemical yield, and O-[1-11C]acetyl-L-carnitine and O-[2-11C] acetyl-L-carnitine in 70-80% yield, based on [1-11C]acetate or [2-11C]acetate, respectively. By an N-methylation reaction with [11C]methyl iodide, L-[methyl-11C]carnitine was obtained within 30 min, and O-acetyl-L-[methyl-11C]carnitine within 40 min, giving a decay-corrected radiochemical yield of 60% and 40-50%, respectively, based on [11C]methyl iodide. Initial data of the kinetics of the different 11C-labelled L-carnitine and acetyl-L-carnitines in renal cortex of anaesthetized monkey (Macaca mulatta) are presented.
本文描述了使用乙酰辅酶A合成酶和肉碱乙酰转移酶，在乙酰基的1-或2-位或肉碱的N-甲基位标记有¹¹C的L-肉碱、O-乙酰辅酶A和O-乙酰-L-肉碱的合成方法。总合成时间为45分钟，基于[1-¹¹C]乙酸盐或[2-¹¹C]乙酸盐，分别以60-70%的衰变校正放射化学产率获得O-[1-¹¹C]乙酰辅酶A和O-[2-¹¹C]乙酰辅酶A，以及以70-80%的产率获得O-[1-¹¹C]乙酰-L-肉碱和O-[2-¹¹C]乙酰-L-肉碱。通过与[¹¹C]甲基碘进行N-甲基化反应，在30分钟内获得L-[甲基-¹¹C]肉碱，在40分钟内获得O-乙酰-L-[甲基-¹¹C]肉碱，基于[¹¹C]甲基碘，其衰变校正放射化学产率分别为60%和40-50%。本文还给出了麻醉猴（猕猴）肾皮质中不同¹¹C标记的L-肉碱和乙酰-L-肉碱动力学的初步数据。
