Source:http://linkedlifedata.com/resource/pubmed/id/19577467
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
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pubmed:dateCreated |
2009-7-29
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pubmed:abstractText |
A new dopamine transporter (DAT) ligand, (E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4'-methyl-phenyl) nortropane (FE-PE2I, 6), derived from PE2I (1), was prepared and found to be a potent inhibitor of rodent DAT in vitro. Compound 6 was radiolabelled with fluorine-18 (t(1/2)=109.8 min) for PET studies in monkeys. In vivo PET measurements showed a regional distribution in brain that corresponds to the known distribution of DAT. This binding was specific, reversible and the kinetics of [(18)F]6 binding in brain were faster than for its lead compound, [(11)C]1. The possible presence of a hydroxymethyl-radiometabolite formed by oxidation in the 3beta-benzylic position of [(18)F]6 warrants further detailed evaluation of the metabolism of [(18)F]6. [(18)F]6 is a potential radioligand for imaging DATs in the human brain with PET.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Plasma Membrane Transport...,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Nortropanes,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4843-5
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pubmed:meshHeading |
pubmed-meshheading:19577467-Animals,
pubmed-meshheading:19577467-Brain,
pubmed-meshheading:19577467-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:19577467-Fluorine Radioisotopes,
pubmed-meshheading:19577467-Haplorhini,
pubmed-meshheading:19577467-Humans,
pubmed-meshheading:19577467-Isotope Labeling,
pubmed-meshheading:19577467-Kinetics,
pubmed-meshheading:19577467-Nortropanes,
pubmed-meshheading:19577467-Positron-Emission Tomography,
pubmed-meshheading:19577467-Radiopharmaceuticals,
pubmed-meshheading:19577467-Rats
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis, radiolabeling and preliminary in vivo evaluation of [18F]FE-PE2I, a new probe for the dopamine transporter.
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pubmed:affiliation |
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm, Sweden. magnus.schou@astrazeneca.com
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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