Fluorine-18-FPCT: A PET radiotracer for imaging dopamine transporters

Academic Article

Abstract

  • Fluorine-18-labeled 2β-carbomethoxy-3β-(4-chlorophenyl)-8-(-3- fluoropropyl)nortropane (FPCT) has been synthesized as a new dopamine transporter imaging agent. Methods: Fluorine-18 was introduced into 2β- carbomethoxy-3β-(4-chlorophenyl)-8-[-3-fluoropropyl) nortropane by preparation of 1-[18F]fluoro-3-iodopropane followed by alkylation of 2β- carbomethoxy-3β-(4-chlorophenyl)nortropane. Results: Tissue distribution studies in rats with [18F]FPCT showed high striatal uptake (0.70% dose/g at 60 min; 0.38% dose/g at 120 min) and good striatal-to-cerebellum ratios (5.5 at 60 min; 6.2 at 120 min). Imaging studies in rhesus monkeys (n = 2) with [18F]FPCT showed high uptake and retention in the putamen (P) (P = 0.03%- 0.12% dose/g; at 115 min) and good putamen-to-cerebellum ratios of 3.40-3.43 at 115 min. Plasma metabolites were analyzed in rhesus monkeys (n = 2) by ether extraction and HPLC. The radioactivity in the ether-extractable fraction displayed a single peak that corresponded on HPLC to unmetabolized authentic FPCT. Conclusion: These results suggest that [18F]FPCT is an excellent candidate for PET imaging of dopamine transporters.
  • Authors

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    Author List

  • Goodman MM; Keil R; Shoup TM; Eshima D; Eshima L; Kilts C; Votaw J; Camp VM; Votaw D; Smith E
  • Start Page

  • 119
  • End Page

  • 126
  • Volume

  • 38
  • Issue

  • 1