Livni E, Elmaleh D R, Levy S, Brownell G L, Strauss W H
J Nucl Med. 1982 Feb;23(2):169-75.
We have tagged heptadecanoic acid with C-11 at the carboxyl group and have inserted a methyl radical in the beta position to inhibit beta oxidation of the fatty acid; we have then explored the tracer's potential as an indicator of myocardial metabolism for use with the positron tomograph. In this preliminary evaluation, biodistribution studies were made in rats and dogs, and imaging of normal and infarcted dogs was performed. At 30 min the tissue distribution studies in rats and dogs showed, respectively, 1.9% and 8.3% uptake in the heart. Sequential images of the canine heart exhibited a remarkable uptake, peaking at 16-18 min and retaining the same level of activity over the one-hour study period. Images of the heart after LAD ligation showed an area of diminished uptake corresponding to the region of infarction. Thus this agent has the basic properties required for potential use in the assessment and quantitation of free fatty-acid metabolism in the heart in a manner similar to the measurement of glucose metabolism in the brain with 2-[18F]fluoro-3-deoxy-D-glucose.
我们已在羧基处用C-11标记了十七烷酸,并在β位插入了一个甲基以抑制脂肪酸的β氧化;然后我们探索了该示踪剂作为心肌代谢指标与正电子断层扫描仪配合使用的潜力。在这项初步评估中,对大鼠和狗进行了生物分布研究,并对正常和梗死的狗进行了成像。在30分钟时,大鼠和狗的组织分布研究分别显示心脏摄取率为1.9%和8.3%。犬心脏的连续图像显示摄取显著,在16 - 18分钟达到峰值,并在一小时的研究期间保持相同的活性水平。左冠状动脉前降支结扎后心脏的图像显示摄取减少的区域与梗死区域相对应。因此,该试剂具有以类似于用2-[18F]氟-3-脱氧-D-葡萄糖测量脑葡萄糖代谢的方式潜在用于评估和定量心脏游离脂肪酸代谢所需的基本特性。