Evaluation of 3H-paroxetine as a radioligand for in vivo study of 5-hydroxytryptamine uptake sites in mouse brain.
The distribution of radioactivity in the mouse brain after intravenous administration of 3H-paroxetine was in the order (highest to lowest) hypothalamus greater than cerebral cortex greater than cerebellum. The radioactivity in the hypothalamus and cerebral cortex after injection of 3H-paroxetine was significantly decreased by treatment with 6-nitroquipazine or paroxetine. HPLC and TLC analyses show that no radioactive metabolites were found in the mouse brain 3 h after intravenous administration of 3H-paroxetine. The present results indicate that 3H-paroxetine would be a suitable radioligand for in vivo study of 5-HT uptake sites in mouse brain.
Hashimoto
K
K
Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, University of Fukuyama, Japan.
Goromaru
T
T
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D005069:Evaluation Studies as Topic; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D017374:Paroxetine; D010880:Piperidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014316:Tritium / Q000008:administration & dosage
D010880:Piperidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014316:Tritium; D017374:Paroxetine