de Groot T, Maris B, Boonen C, Bormans G, Mortelmans L, Eisenhut M, Verbruggen A
Laboratory for Radiopharmaceutical Chemistry FFW, University Hospital Gasthuiseberg, Leuven, Belgium.
Nucl Med Biol. 1997 Jul;24(5):461-4. doi: 10.1016/s0969-8051(97)00009-7.
A phenylene moiety in the chain of fatty acids was expected to impair metabolic degradation. Three phenoxy-containing [11C]carboxyl-labelled fatty acids were synthesized and evaluated in mice and an in vivo tissue distribution study. Of these three, 1[11C]-3-(p-dodecyloxyphenyl)propionic acid (C12C3) showed the most favourable uptake in the myocardium: 1.2% of the injected dose at 30 min p.i., vs. 0.6% for [11C]palmitate. The metabolic stability of C12C3 and [11C]palmitate was assessed by determining the amount of exhaled [11C]CO2 during a 30-min interval after injection. It was found that the phenoxy moiety in the gamma-position did not prevent the metabolic degradation of C12C3: After 30 min 20.7% of the injected dose was exhaled as [11C]CO2 vs. 12.7% for [11C]palmitate.
脂肪酸链中的亚苯基部分预计会损害代谢降解。合成了三种含苯氧基的[11C]羧基标记脂肪酸，并在小鼠中进行评估以及开展了一项体内组织分布研究。在这三种脂肪酸中，1-[11C]-3-(对十二烷氧基苯基)丙酸（C12C3）在心肌中的摄取最为理想：注射后30分钟时摄取量为注射剂量的1.2%，而[11C]棕榈酸盐为0.6%。通过测定注射后30分钟间隔内呼出的[11C]CO2量来评估C12C3和[11C]棕榈酸盐的代谢稳定性。结果发现，γ位的苯氧基部分并未阻止C12C3的代谢降解：30分钟后，注射剂量的20.7%以[11C]CO2形式呼出，而[11C]棕榈酸盐为12.7%。
