发明名称 |
Enantiomers of 2'-Fluoralky1-6-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 radiolabelled 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.
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申请公布号 |
US7998962(B2) |
申请公布日期 |
2011.08.16 |
申请号 |
US20100887782 |
申请日期 |
2010.09.22 |
申请人 |
THE UNIVERSITY OF MONTANA |
发明人 |
GERDES JOHN M.;BOLSTAD DAVID B.;KUSCHE BRIAN R. |
分类号 |
A61K31/496;C07D401/04 |
主分类号 |
A61K31/496 |
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