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No-Carrier-Added N-(3-[¹⁸F]Fluoropropyl)spiroperidol: Biodistribution in Mice and Tomographic Studies in a Baboon

Chyng-Yann Shiue, Lan-Qin Bai^*, Ren-Rui Teng, Carroll D. Arnett and Alfred P. Wolf

Department of Chemistry, Brookhaven National Laboratory, Upton, New York

Correspondence: For reprints contact: C.-Y. Shiue, PhD, Dept. of Chemistry, Brookhaven National Laboratory, Upton, NY 11973.

ABSTRACT

Two potential radioligands, no-carrier-added (NCA) N-(2-[¹⁸F]fluoroethyl)spiroperidol (3) and N-(3-[¹⁸F]fluoropropyl)spiroperidol (4) have been synthesized for PET imaging of dopamine receptors in humans. Compounds 3 and 4 were synthesized by N-alkylation of spiroperidol with NCA 1-bromo-2-[¹⁸F]-fluoroethane (2b), 1-[¹⁸F]fluoro-3-iodopropane (2c) and 1-bromo-3-[¹⁸F]fluoropropane (2d) respectively. The biodistribution of 4 in mice showed that the mouse brain uptake of radioactivity was similar to that of [¹⁸F]-N-methylspiroperidol (1.1% of the administered dose), but the activity in bone (femur) increased with time. The kinetic distribution of compound 4 in baboon brain was similar to that of [¹⁸F]-N-methylspiroperidol, and the striatal accumulation of radioactivity was also blocked stereosetectively by butaclamol. The ratio of striatum to cerebellum radioactivities at 3 hr after injection was 5.9. Analysis of the metabolic stability of 4 in mouse brains for 1 hr indicated that, like [¹⁸F]-N-methylspiroperidol, it is relatively stable to metabolic transformation in the central nervous system. These results suggest that compound 4 may be a useful radioligand for PET studies of the dopamine receptor in humans.

FOOTNOTES

^* Permanent address: Visiting Scholar from Institute of Atomic Energy, Beijing, People's Republic of China.

Permanent address: Visiting Scholar from Institute of Modern Physics, Academia Sinica, Lanzhou, People's Republic of China.