长链脂肪酸衍生物99Tcm-MAMA-(CH2)nCOOH的制备和生物分布

长链脂肪酸衍生物⁹⁹Tc^m-MAMA-(CH₂)_nCOOH的制备和生物分布

摘要: 以短链二酸和N2S2类配体（MAMA）为起始原料，合成了4个长链脂肪酸衍生物MAMA-(CH₂)_nCOOH（n=14,15,16,17），通过与⁹⁹Tc^m-GH在沸水浴中加热30 min完成配体交换反应，实现了99Tcm的标记，其标记率均大于90%。正常小鼠的生物分布数据显示这4个标记物在心肌中均有一定的摄取（5 min时的放射性摄取百分数依次为5.73、5.52、4.82和4.03%ID•g－1），但血本底较高，而且血清除较慢，标记物能否参与脂肪酸尚需进一步研究。

Abstract: Four long-chain fatty acid analogues MAMA-(CH₂)_nCOOH (n=14,15,16,17) are synthesized from medium-chain fatty acid and monoamine-monoamide dithiol ligand (MAMA). ⁹⁹Tc^m complexes (⁹⁹Tc^m-MAMA-FA) are prepared by ligand-exchange reaction with ⁹⁹Tc^m-GH in boiling water bath for the development of 99Tcm labeled fatty acid metabolism imaging agent ，and their biodistributions in normal mice are studied. The results indicate that the four labeled compounds have low initial heart uptake，but they have high blood uptake and slow blood clearance.