Ishiwata K, Ido T, Yanai K, Kawashima K, Miura Y, Monma M, Watanuki S, Takahashi T, Iwata R
J Nucl Med. 1985 Jun;26(6):630-6.
Carbon-11 (11C) pargyline, which is a suicide inactivator of Type B monoamine oxidase (MAO), was synthesized by the reaction of N-demethylpargyline with 11CH3I. Biodistribution was investigated in mice, and positron tomographic images of the heart and lung in a rabbit were obtained. The distribution of 11C after administration of [11C]pargyline was measured in several organs and blood at various time intervals. After 30 min its concentrations in the organs were constant. Subcellular distribution studies in the brain, lung, liver, and kidney showed that 59-70% of the 11C became acid-insoluble and 9-33% was present in the crude mitochondrial fraction at 60 min after injection. However, a high loading dose influenced the subcellular distribution but had little effect on tissue distribution. The uptakes of the 11C in each organ except for the kidney and spleen seemed to correlate with the in vitro enzymatic activity of Type B MAO. At high loading dose a nonspecific uptake was observed.
碳-11（¹¹C）帕吉林是B型单胺氧化酶（MAO）的自杀性失活剂，由N-去甲基帕吉林与¹¹CH₃I反应合成。研究了其在小鼠体内的生物分布，并获得了兔子心脏和肺部的正电子断层图像。在不同时间间隔测量了给予[¹¹C]帕吉林后¹¹C在多个器官和血液中的分布。30分钟后，其在器官中的浓度保持恒定。在脑、肺、肝和肾中进行的亚细胞分布研究表明，注射后60分钟，59 - 70%的¹¹C变为酸不溶性，9 - 33%存在于粗线粒体组分中。然而，高剂量影响亚细胞分布，但对组织分布影响较小。除肾和脾外，各器官对¹¹C的摄取似乎与B型MAO的体外酶活性相关。在高剂量时观察到非特异性摄取。
