Technetium-99m-labeled long chain fatty acid analogues metabolized by beta-oxidation in the heart |
| |
Authors: | Uehara Tomoya Uemura Tomoe Hirabayashi Seiji Adachi Sayaka Odaka Kenichi Akizawa Hiromichi Magata Yasuhiro Irie Toshiaki Arano Yasushi |
| |
Affiliation: | Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|