This paper describes the radiosynthesis of [C-11]CGP62349, a potential ligand to assess GABA, receptors in vivo. C-11 was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey, revealing negligible blood brain barrier penetration and brain uptake, thus prompting us to search for a new target structure with a better lipophilicity. NUCL MED BIOL 27;6:565-569, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.
Todde, S., Moresco, R., Frostl, W., Stampf, P., Matarrese, M., Carpinelli, A., et al. (2000). Synthesis and in vivo evaluation of [C-11]CGP62349, a new GABA(B) receptor antagonist. NUCLEAR MEDICINE AND BIOLOGY, 27(6), 565-569 [10.1016/S0969-8051(00)00124-4].
Synthesis and in vivo evaluation of [C-11]CGP62349, a new GABA(B) receptor antagonist
TODDE, SERGIO CAMILLO;MORESCO, ROSA MARIA;MAGNI, FULVIO;KIENLE, MARZIA DONATELLA;FAZIO, FERRUCCIO
2000
Abstract
This paper describes the radiosynthesis of [C-11]CGP62349, a potential ligand to assess GABA, receptors in vivo. C-11 was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey, revealing negligible blood brain barrier penetration and brain uptake, thus prompting us to search for a new target structure with a better lipophilicity. NUCL MED BIOL 27;6:565-569, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.
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