Development of New Noninvasive Methods of Functional Imaging Using Biologically Active Substances Labelled with Positron Emitting Radionuclides

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1. Chemical ResearchAn efficient synthesis of[fluoroacetyl-^<18>F]fluoromelatonin (1) has been established. The desired isotope (1) was obtained in a 26.7% radiochemical yield. The purity, specific activity and the total time required for its synthesis are>98%, 540mCi/mmol and ca.90 min, respectively. N^<omega>-[^<18>F]Fluoroacetylserotonin (2) was also synthesized under similar conditions in 22.6% radiochemical yield. The purity and specific activity of the hormone (2) are>98% and 600mCi/mmol, respectively.2. Medical ResearchWe have examined the feasibility of positron labelled radiopharmaceuticals for functional imaging.(1). Tissue distribution of (1) has been studies using mice. The distribution was similar to that of iodolabelled melatonin which has been reported previously. It is suggested that (1)may be a useful tracer for studying the correlation of melatonin metabolism and circadian rhythm.(2). We have studied the tumor imaging with PET using N-[^<18>F]Fluoroacetyl-D-glucosamine(3). Sugar(3) was intravenously injected through the ear vein to a Japanese white rabbit bearing a VX2 tumor in the thigh, and PET imaging was performed. Tumor was clearly visualized using (3).(3) .Clinical PET sudy demonstrated the usefulness of 2-Deoxy-2-[^<18>F]fluoro-D-galactose for the detection of extrahepatic metastasis of hepatoma.