Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2012, Vol. 23 ›› Issue (1): 40-46 doi: 10.13538/j.1001-8042/nst.23.40-46

• RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICIN • Previous Articles     Next Articles

Semi-automated synthesis,validation and microPET imaging of 18F-FP-DTBZ as a vesicular monoamine transporter ligand

CHEN Zhengping LIU Chunyi LI xiaomin TANG Jie TAN Cheng HUANG Hongbo YU Huixin LUO Shineng   

  1. Key Laboratory of Nuclear Medicine,Ministry of Health,Jiangsu Key Laboratory of Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063,China
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CHEN Zhengping, LIU Chunyi, LI xiaomin, TANG Jie, TAN Cheng, HUANG Hongbo, YU Huixin, LUO Shineng. Semi-automated synthesis,validation and microPET imaging of 18F-FP-DTBZ as a vesicular monoamine transporter ligand.Nuclear Science and Techniques, 2012, 23(1): 40-46     doi: 10.13538/j.1001-8042/nst.23.40-46

Abstract:

This work was to develop a semi-automated synthesis of 18F-9-fluoropropyl-9-desmethyl-DTBZ (18F-FP-DTBZ) and validate its potential as a vesicular monoamine transporter 2 (VMAT2) ligand.18F-FP-DTBZ was synthesized by a semi-automated procedure in a 21-35% yield without decay correction and with a radiochemical purity of >98%.Bioistribution in rats exhibited a favorable brain uptakes of the ligand (0.31±0.04 ID% at 60min post injection,n=8).The highest radioactivity located in VMAT2 enriched striatal tissue.The target-to-nontarget ratio (striatum/cerebellum,ST/CB) was 4.81±0.84.Blocking studies implied that striatum uptake could be blocked by DTBZ (a VMAT2 inhibitor) but could not by CFT (a dopamine transporter inhibitor).MicroPET imaging with 18F-FP-DTBZ in normal rats gave high quality images in which high radioactivity were observed in the striatal tissue.Time-and-activity curves revealed good retention in the target (striatum) and rapid clearance in the background (cerebellum),which resulted in a maximum ST/CB ratio of 5.08±0.81 (n=3) in 80-120min.By contrast,the 6-hydroxydopamine unilateral lesioned rats gave asymmetrical striata images with higher 18F-FP-DTBZ concentration on the unlesioned side (unlesioned-ST/CB=5.21±0.38,n=3) than the lesioned (lesioned-ST/CB=2.34±0.51).The results validated that 18F-FP-DTBZ is a favorable PET ligand binding to VMAT2.

Key words: VMAT2, Imaging agent, 18F-FP-DTBZ, Synthesis, Biodistribution, MicroPET, Parkinson's disease