Preparation and Biological Evaluation of Novel ¹⁸F-labeled Phosphonuim Cation for Myocardial Perfusion Imaging with PET

In order to develop new PET myocardial perfusion imaging agent, a novel ¹⁸F labeled phosphonium cation: (3-(¹⁸Ffluoromethyl)benzyl) tris (2, 6-dimethoxyphenyl) phosphonium salt, ¹⁸F-2, had been designed and prepared. Biological evaluation of ¹⁸F-2 had been performed in Kunming normal mice. ¹⁸F-2 was obtained by a simple one-pot method and the radiochemical yield was (31±3)%. The total radio-synthesis time was less than 60 min and the radiochemical purity of final radiotracer was more than 95%. The biodistribution of ¹⁸F-2 displayed a high heart uptake and good retention. The heart uptake of ¹⁸F-2 at 5 and 60 min post-injection were (53.88±7.45)%ID/g and (23.93±3.28)%ID/g, respectively. ¹⁸F-2 exhibited low radio-accumulation in non-target tissues and rapid clearance in liver, lung and blood. The heart to liver, heart to lungs and heart to blood ratio values were 3.99, 3.80 and 9.17, respectively. The results indicated that ¹⁸F-2 could be as a promising myocardial perfusion imaging agent for PET imaging.