Technetium-99m-labeled long chain fatty acid analogues metabolized by beta-oxidation in the heart.
Technetium-99m-labeled long chain fatty acid analogues metabolized by beta-oxidation in the heart.
复制标题
DOI：
10.1021/jm061017g
复制
发表时间：
2007-01
影响因子：
7.3
通讯作者：
T. Uehara;Tomoe Uemura;S. Hirabayashi;Sayaka Adachi;K. Odaka;H. Akizawa;Y. Magata;T. Irie;Y. Arano
中科院分区：
文献类型：
--
作者：
T. Uehara;Tomoe Uemura;S. Hirabayashi;Sayaka Adachi;K. Odaka;H. Akizawa;Y. Magata;T. Irie;Y. Arano
99 mTc标记的脂肪酸类似物在心肌中通过β-氧化代谢的发展构成了一个未解决的挑战。根据我们最近的发现，[188 Re]三羰基（环戊二烯基碳酸酯）锝（[188 Re]CpTR-COOH）被认为是一种芳香族化合物，并在体内代谢，将[99 mTc]环戊二烯基三羰基锝（[99 mTc]CpTT）与十五烷酸的ω-位结合，制备[99 mTc]CpTT-PA。大鼠注射[99 mTc]CpTT-PA后1 min心肌蓄积最大，心血比为3.85%ID/g，10 min为4.60。使用离体Langendorff灌注大鼠心脏的代谢研究表明，约67%的灌注[99 mTc]CpTT-PA被掺入，[99 mTc] CpTT-PA β-氧化6个循环后的代谢物[99 mTc] CpTT-丙酸被检测为灌注液和心肌中的主要放射性代谢物。这些结果表明，[99 mTc]CpTT-PA被识别，运输，并作为一种长链脂肪酸类似物在心肌中的能量产生代谢。
The development of 99mTc-labeled fatty acid analogues metabolized by beta-oxidation in the myocardium constitutes an unsolved challenge. On the basis of our recent findings that [188Re]tricarbonyl(cyclopentadienylcarbonate)rhenium ([188Re]CpTR-COOH) was recognized as an aromatic compound and was metabolized as such in the body, [99mTc]cyclopentadienyltricarbonyltechnetium ([99mTc]CpTT) was conjugated at the omega-position of pentadecanoic acid to prepare [99mTc]CpTT-PA. When injected into rats, [99mTc]CpTT-PA exhibited the maximum myocardial accumulation and heart-to-blood ratio of 3.85 %ID/g at 1 min and 4.60 at 10 min postinjection, respectively. The metabolic study using isolated Langendorff perfused rat hearts demonstrated that approximately 67% of perfused [99mTc]CpTT-PA was incorporated and [99mTc]CpTT-propionic acid, the metabolite after six cycles of beta-oxidation of [99mTc]CpTT-PA, was detected as the major radiometabolite in the perfusate and myocardium. These findings indicate that [99mTc]CpTT-PA was recognized, transported, and metabolized as a long chain fatty acid analogue for energy production in the myocardium.