Synthesis and biodistribution of 18F-labeled pyridyl pyridaben analogues

doi:10.3969/j.issn.1006-7795.2013.01.003

Abstract

Abstract:

Objective A fluorine-18 labeled pyridazinone derivative: 4-chloro-2-tert-butyl-5-[6-[4-[2-[2-[2-[¹⁸F]fluroethoxy]ethoxy]ethoxy]-1H-1,2,3-triazol-1-yl]methyl]-2-pyridinyl]methoxy]-3(2H)-pyridazinone ([¹⁸F]FPTP-P3) was designed and prepared, and its potential as a myocardial perfusion imaging agent was evaluated. Methods [¹⁸F]FPTP-P3 was prepared by substituting tosyl of precursor with ¹⁸F. The tracer was evaluated by stability study, octanol/water partition coefficient and biodistribution study. Results The total radio-synthesis time was 70-90 min, typical decay-corrected radiochemical yield was 36±5.6%, and the radiochemical purity (RCP) was>98% after purification. It is a lipophilic compound, and stable in water for 3 h. The results of biodistribution study in mice showed that [¹⁸F]FPTP-P3 had certain initial heart uptake and the clearance of liver was very fast as well. However the retention of heart uptake was not ideal.Conclusion [¹⁸F]FPTP-P3 is not suitable for heart imaging in vivo.

Key words: [¹⁸F]FPTP-P3, pyridaben, heart uptake, biodistribution

CLC Number:

R392
Q2

MOU Tiantian, ZHANG Xianzhong, WANG Qian, PENG Cheng, MA Yunchuan, MI Hongzhi. Synthesis and biodistribution of ¹⁸F-labeled pyridyl pyridaben analogues[J]. Journal of Capital Medical University, 2013, 34(1): 11-17.

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URL: https://journal03.magtech.org.cn/Jweb_sdykdxxb/EN/10.3969/j.issn.1006-7795.2013.01.003

https://journal03.magtech.org.cn/Jweb_sdykdxxb/EN/Y2013/V34/I1/11

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Synthesis and biodistribution of ¹⁸F-labeled pyridyl pyridaben analogues

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