V. J. Majo, R. Parsey, J. Prabhakaran
Mar 15, 2008
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
4-[3-[4-(2-Methoxyphenyl)piperazin-1-yl]propoxy]-4-aza-tricyclo[5.2.1.02,6]dec-8-ene-3,5-dione (4), a potent and selective 5-HT1A agonist, was labeled by 11C-methylation of the corresponding desmethyl analogue 3 with 11C-methyl triflate. The precursor molecule 3 was synthesized from commercially available endo-N-hydroxy-5-norbornene-2,3-dicarboximide in two steps with an overall yield of 40%. Radiosynthesis of 11C-4 was achieved in 35 min in 20±5% yield (n=6) at the end of synthesis with a specific activity of 2600±250 Ci/mmol. In vivo positron emission tomography (PET) studies in baboon revealed rapid uptake of the tracer into the brain. However, lack of specific binding indicates that 11C-4 is not useful as a 5-HT1A agonist PET ligand for clinical studies. Copyright © 2008 John Wiley & Sons, Ltd.