The Development of New Radiohalagenated Cocaine Analogues for Inviva Duty of Dopamine Reuptdae in New Radegenative Diseases
Fluorine-18-labeled 2{beta}-carbomethoxy-3{beta}-(4-chlorophenyl)-8-(3-fluoropropyl)nortropane (FPCT) has been synthesized as a new dopamine transporter imaging agent. Fluorine-18 was introduced into 2{beta}-carbomethoxy-3{beta}-(4-chlorophenyl)-8-[-3-fluoropropy] nortropane by preparation of 1-[{sup 18}F]fluoro-3-iodopropane followed by alkylation of 2{beta}-carbomethoxy-3{beta}-(4-chlorophenyl)nortropane. Tissue distribution studies in rats with [{sup 18}F]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 [{sup 18}F]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 HLPC. The radioactivity in the ether-extractable fraction displayed a single peak that corresponded on HPLC to unmetabolized authentic FPCT. These results suggest that [{sup 18}F]FPCT is an excellent candidate for PET imaging of dopamine transporters. 32 refs., 7 figs., 3 tabs.
- Research Organization:
- Oak Ridge National Laboratory (ORNL), Oak Ridge, TN
- Sponsoring Organization:
- USDOE
- DOE Contract Number:
- FG05-93ER61737
- OSTI ID:
- 430943
- Report Number(s):
- DOE/ER/61737; 93080402
- Country of Publication:
- United States
- Language:
- English
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