M. Sakata, J. Toyohara, K. Ishiwata
Aug 1, 2010
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NeuroImage
Abstract
Introduction: Since glycine acts as a co-agonist at the NMDA receptors, glycine transporter 1 (GlyT-1) has been an attractive target in PET studies of recent date. For visualizing of the distribution and density of GlyT-1, non-sarcosine-based GlyT-1 inhibitors, such as [C]GSK9311145 [1], are considered to be promising compounds. In this study, three carbon-11-labeled N-((S)-1-((S)-1-methylpiperidin-2-yl)ethyl)acetamide derivatives, 2-chloro-3-(trifluoromethyl)-N-((S)-((S)-1-[C]methylpiperidin-2-yl)(thiophen-3-yl)methyl)benzamide ([C]SA1), N-((S)-((S)1-[C]methylpiperidin-2-yl)(phenyl)methyl)thiophene-2-carboxamide ([C]SA2), and 2-chloro-3-(trifluoromethyl)-N-((S)-((S)-1-[C] methylpiperidin-2-yl)(phenyl)methyl)benzamide ([C]SA3) were investigated by conscious monkey PET studies. Our companion paper presents the radiosynthesis and the rodent study of these radioligands.