Abstract
[11C]-labeled form of ten A2a 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 A2a receptors.
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T. Márián, I. Boros, Z. Lengyel, L. Balkay, G. Horváth, M. Emri, É. Sarkadi, A. J. Szentmiklósi, I. Fekete, L. Trón, Appl. Radiation Isotopes, 50 (1999) 887.
J. W. Daly, J. Med. Chem., 25 (1982) 197.
K. Ishiwata, R. Furuta, J. Shimada, S. Ishi, K. Endo, F. Suzuki, M. Senda, Appl. Radiation Isotopes, 46 (1995) 1009.
K. Ishiwata, J. Noguchi, H. Toyama, Y. Sakiyama, N. Koike, S. Ishi, K. Oda, K. Endo, F. Suzuki, M. Senda, Appl. Radiation Isotopes, 47 (1996) 507.
B. B. Fredholm, M. P. Abbracchio, G. Burnstock, J. W. Daly, T. K. Harden, K. A. Jacobson, P. Leff, M. Williams, Pharmacol. Rev., 46 (1994) 143.
K. A. Jacobson, O. Nikodijevic, W. Padgett, C. Gallo-Rodriguez, M. Maillard, P. J. Van Galen, J. W. Daly, FEBS Lett., 323 (1993a) 141.
K. A. Jacobson, C. Gallo-Rodriguez, N. Melman, B. Fischer, M. Maillard, A. Van Bergen, P. J. Van Galen, J. Y. Karton, Med. Chem., 36 (1993b) 1333.
Y. Nonaka, J. Shimada, H. Nonaka, N. Koike, N. Aoki, A. Kobayashi, H. Kase, K. Yamaguchi, F. Suzuki, J. Med. Chem., 36 (1993) 3731.
É. Sarkadi, Z. Kovács, L. Andó, F. Szelecsényi, Radiochim. Acta, 76 (1997) 197.
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Boros, I., Horváth, G., Lehel, S. et al. [11C]-labeling of some caffeine derivatives for mapping adenosine A2a receptors by PET technique. J Radioanal Nucl Chem 242, 309–312 (1999). https://doi.org/10.1007/BF02345557
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DOI: https://doi.org/10.1007/BF02345557