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Synthesis,radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine,a potential radioligand for the serotonin transporter |
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| Authors: | Sandell Johan Yu Meixiang Emond Patrick Garreau Lucette Chalon Sylvie Någren Kjell Guilloteau Denis Halldin Christer |
| Affiliation: | a Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-171 76, Stockholm, Sweden b Turku PET Centre, Radiopharmaceutical Chemistry Laboratory, Porthaninkatu 3, FIN-20500, Turku, Finland c INSERM U316, Laboratoire Biophysique Médicale et Pharmaceutique, Faculté des Sciences Pharmaceutiques, Université François Rabelais, 31 avenue, Monge, F-37200 Tours, France |
| Abstract: | 5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a Kd=51±7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography. |
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