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[11C]-labeling of some caffeine derivatives for mapping adenosine A2a receptors by PET technique

Authors:	I Boros G Horváth S Lehel T Márián Z Kovács J Szentmiklósi G Tóth L Trón

Institution:	(1) PET Centre, University Medical School of Debrecen, Nagyerdei krt 98, H-4012 Debrecen, Hungary;(2) Department of Pharmacology, University Medical School of Debrecen, Nagyerdei krt 98, H-4012 Debrecen, Hungary;(3) Institute of Nuclear Research of the Hungarian Academy of Science, Bem tér 18/C, H-4026 Debrecen, Hungary;(4) Institute of Isotopes Co. Ltd., P.O. Box 851, H-1525 Budapest, Hungary

Abstract:	¹¹C]-labeled form of ten A_2a adenosine receptor specific 8-styryl-7-methyl-xanthine derivatives (¹¹C]-caffeines) were synthesised by N-methylation of the corresponding 8-styryl-xanthine derivatives using ¹¹C]-methyl iodide in optimized reaction conditions. The results show that the ¹¹C]-methylations take place with excellent radiochemical yields (35–93%), and can be utilised easily in online preparations. These labeled ligands may facilitate the positron emission tomographic (PET) investigation of adenosine A_2a receptors.

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