Fluorine-18-FPCT: a PET radiotracer for imaging dopamine transporters
| Autor: | M M, Goodman, R, Keil, T M, Shoup, D, Eshima, L, Eshima, C, Kilts, J, Votaw, V M, Camp, D, Votaw, E, Smith, M P, Kung, E, Malveaux, R, Watts, M, Huerkamp, D, Wu, E, Garcia, J M, Hoffman |
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| Rok vydání: | 1997 |
| Předmět: |
Male
Dopamine Plasma Membrane Transport Proteins Fluorine Radioisotopes Membrane Glycoproteins Nortropanes Brain Contrast Media Membrane Transport Proteins Nerve Tissue Proteins Macaca mulatta Rats Rats Sprague-Dawley Animals Female Tissue Distribution Radiopharmaceuticals Carrier Proteins Tomography Emission-Computed |
| Zdroj: | Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 38(1) |
| ISSN: | 0161-5505 |
| Popis: | 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-fluoropropyl) nortropane by preparation of 1-[18F]fluoro-3-iodopropane followed by alkylation of 2 beta-carbomethoxy-3 beta-(4-chlorophenyl)nortropane.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.These results suggest that [18F]FPCT is an excellent candidate for PET imaging of dopamine transporters. |
| Databáze: | OpenAIRE |
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