title: Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter.
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 K(d)=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.
authors.affiliation: Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-171 76 Stockholm, Sweden. johan.sandell@pet.uu.se
authors.forename: Johan
authors.initials: J
authors.lastname: Sandell
authors.forename: Meixiang
authors.initials: M
authors.lastname: Yu
authors.forename: Patrick
authors.initials: P
authors.lastname: Emond
authors.forename: Lucette
authors.initials: L
authors.lastname: Garreau
authors.forename: Sylvie
authors.initials: S
authors.lastname: Chalon
authors.forename: Kjell
authors.initials: K
authors.lastname: Någren
authors.forename: Denis
authors.initials: D
authors.lastname: Guilloteau
authors.forename: Christer
authors.initials: C
authors.lastname: Halldin
mesh_terms: D000818:Animals; D002250:Carbon Radioisotopes; D002352:Carrier Proteins / Q000037:antagonists & inhibitors; D008024:Ligands; D008562:Membrane Glycoproteins / Q000037:antagonists & inhibitors; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D017397:Prefrontal Cortex / Q000378:metabolism; D011814:Quipazine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D050486:Serotonin Plasma Membrane Transport Proteins; D013329:Structure-Activity Relationship; D014316:Tritium
chemical_list: C471420:5-methyl-6-nitroquipazine; D002250:Carbon Radioisotopes; D002352:Carrier Proteins; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D019275:Radiopharmaceuticals; D012702:Serotonin Antagonists; D050486:Serotonin Plasma Membrane Transport Proteins; C493232:Slc6a4 protein, rat; D014316:Tritium; D011814:Quipazine