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用于心脏代谢成像的镓标记棕榈酸的合成与评估

Synthesis and evaluation of Ga labeled palmitic acid for cardiac metabolic imaging.

作者信息

Jain Akanksha, Mathur Anupam, Pandey Usha, Sarma Haladhar Dev, Dash Ashutosh

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India.

Radiopharmaceuticals Program, Board of Radiation and Isotope Technology, Navi Mumbai 400703, India.

出版信息

Appl Radiat Isot. 2018 Oct;140:35-40. doi: 10.1016/j.apradiso.2018.06.003. Epub 2018 Jun 5.

Abstract

This work evaluates the potential of a Ga labeled long chain 16C fatty acid for cardiac metabolic imaging. For radiolabeling with Ga, hexadecanedioic acid was coupled with the chelator p-NH-Bn-NOTA. Under the optimized conditions, NOTA-hexadecanoic acid could be radiolabeled with Ga in ≥95% yields. In biodistribution studies carried out in Swiss mice, Ga-NOTA-hexadecanoic acid showed low myocardial uptake at 2 min p.i. (3.7 ± 1.3%ID/g). While Ga-NOTA-hexadecanoic acid cleared rapidly from non-target organs such as blood, lungs, intestine and kidney, wash out from liver was slow. Radio-HPLC analyses of myocardial extracts of rats injected with Ga-NOTA-hexadecanoic acid confirmed its metabolic transformation in the myocardium.

摘要

这项工作评估了一种镓标记的16碳长链脂肪酸用于心脏代谢成像的潜力。为了用镓进行放射性标记,将十六烷二酸与螯合剂对氨基苄基-NOTA偶联。在优化条件下,NOTA-十六烷二酸可以以≥95%的产率用镓进行放射性标记。在对瑞士小鼠进行的生物分布研究中,Ga-NOTA-十六烷二酸在注射后2分钟时心肌摄取较低(3.7±1.3%ID/g)。虽然Ga-NOTA-十六烷二酸能迅速从血液、肺、肠道和肾脏等非靶器官清除,但从肝脏的清除较慢。对注射了Ga-NOTA-十六烷二酸的大鼠心肌提取物进行的放射性高效液相色谱分析证实了其在心肌中的代谢转化。

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