ENANTIOMERS OF 2'-FLUORALKYL-6-NITROQUIPAZINE AS SEROTONIN TRANSPORTER POSITRON EMISSION TOMOGRAPHY IMAGING AGENTS AND ANTIDEPRESSANT THERAPEUTICS
摘要
Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabeled 2'-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2'-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
申请公布号
WO2007127262(A2)
申请公布日期
2007.11.08
申请号
WO2007US10053
申请日期
2007.04.26
申请人
THE UNIVERSITY OF MONTANA;GERDES, JOHN, M.;BOLSTAD, DAVID, B.;KUSCHE, BRIAN, R.
发明人
GERDES, JOHN, M.;BOLSTAD, DAVID, B.;KUSCHE, BRIAN, R.