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放射性碘化14-(碘苯基)-3-(R,S)-甲基十四烷酸的合成与评价

The synthesis and evaluation of radioiodinated 14-(iodophenyl)-3-(R,S)methyltetradecanoic acid.

作者信息

Elmaleh D R, Livni E, Okada R, Needham F L, Schleuederberg J, Strauss H W

出版信息

Nucl Med Commun. 1985 May;6(5):287-97. doi: 10.1097/00006231-198505000-00007.

DOI:10.1097/00006231-198505000-00007
PMID:4034126
Abstract

Radiohalogenated fatty acids (FA) labelled with gamma-emitting isotopes have a potentially important application in studies of impaired myocardial perfusion and metabolism. Evaluation of straight-chain fatty acids radiolabelled in different positions on the FA chain has been reported by many groups. In this paper we extended our recent studies using the betamethyl branched-chain fatty acid. The synthesis, labelling and preliminary evaluation of 131I- and 123I-14-(iodophenyl)-3-(R,S)methyltetradecanoic acid (I-PBMTA) are reported. This radiolabel concentrates in the mouse myocardium with 16% injected dose g-1 and 11% injected dose g-1 at 15 and 30 min, respectively. The images of the canine heart postinjection indicate a high myocardial extraction of the label with activity retained over an hour. The rate of washout of the activity from the heart was very low. This analogue is a potential agent for myocardial imaging studies.

摘要

用发射γ射线的同位素标记的放射性卤代脂肪酸在心肌灌注和代谢受损的研究中具有潜在的重要应用。许多研究小组报告了对脂肪酸链上不同位置进行放射性标记的直链脂肪酸的评估。在本文中,我们扩展了最近使用β-甲基支链脂肪酸的研究。报告了131I和123I标记的14-(碘苯基)-3-(R,S)-甲基十四烷酸(I-PBMTA)的合成、标记及初步评估。该放射性标记物在小鼠心肌中的聚集量在15分钟和30分钟时分别为每克注射剂量的16%和11%。注射后犬心脏的图像显示该标记物在心肌中的摄取率很高,且活性保留超过一小时。该活性物质从心脏中清除的速率非常低。这种类似物是心肌成像研究的潜在试剂。

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The synthesis and evaluation of radioiodinated 14-(iodophenyl)-3-(R,S)methyltetradecanoic acid.放射性碘化14-(碘苯基)-3-(R,S)-甲基十四烷酸的合成与评价
Nucl Med Commun. 1985 May;6(5):287-97. doi: 10.1097/00006231-198505000-00007.
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