Preparation of [3H]6-nitroquipazine, a potent and selective 5-hydroxytryptamine uptake inhibitor.
The synthesis of 6-nitroquipazine, a very potent and selective 5-hydroxytryptamine (5-HT; serotonin) uptake inhibitor, labeled with tritium is described. High specific activity [3H]6-nitroquipazine could be prepared by the nitration of [3H]quipazine using a mixture of equal volumes of sulfuric acid and nitric acid. The radiochemical yield was approximately 50% based on [3H]quipazine. The radiochemical purity was more than 95% from high performance liquid chromatography(HPLC) and thin layer chromatography(TLC) determinations. [3H]6-Nitroquipazine would be a new suitable radioligand for studying 5-HT transporter complex in brain and platelets.
Hashimoto
K
K
Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, University of Fukuyama, Japan.
Goromaru
T
T
D011804:Quinolines; D011814:Quipazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D012702:Serotonin Antagonists / Q000138:chemical synthesis*; D014316:Tritium
D011804:Quinolines; D012702:Serotonin Antagonists; D014316:Tritium; D011814:Quipazine; C031227:6-nitroquipazine