Synthesis and evaluation of radioiodinated terminal para-iodophenyl-substituted .alpha.- and .beta.-methyl-branched fatty acids
作者:M. M. Goodman、G. Kirsch、F. F. Knapp
DOI:10.1021/jm00369a027
日期:1984.3
long-chain fatty acids. The syntheses and physical properties of 14-(p-iodophenyl)-2(RS)-methyltetradecanoic acid and 15-p-iodophenyl)-3(RS)-methylpentadecanoic acid are described. The radioiodinated agents are of interest as a result of the expected pronounced uptake and prolonged myocardial retention that may result from the inhibition of fatty acid metabolism. Tissue distribution studies in rats
已经开发出用于制备末端对-偶氮苯基取代的α-和β-甲基支化的长链脂肪酸的方法。描述了14-(对碘苯基)-2(RS)-甲基十四烷酸和15-对碘苯基)-3(RS)-甲基十五烷酸的合成和物理性质。由于预期的明显摄取和延长的心肌滞留(可能由抑制脂肪酸代谢所致),使放射性碘化剂受到关注。在具有14-(对-[125I]碘代苯基)-2(RS)-甲基十四烷酸和15-(对-[125I]碘代苯基)-3(RS)-甲基十五烷酸的大鼠中的组织分布研究显示明显的心脏摄取和长时间保留伴随着体内低碘化和高血脂。放射性碘化甲基支链脂肪酸及其非支链类似物对心脏的摄取比较表明,甲基支链脂肪酸的心肌保留度高于非支链类似物。这些结果表明,由于甲基的存在,心肌滞留的机理是由空间或化学抑制这些脂肪酸的代谢所致。