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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1990-3-27
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pubmed:abstractText |
Nisoxetine, a selective and high affinity (IC50 = 1 nM) inhibitor of NE reuptake, has been radiolabeled in high specific activity (greater than 600 Ci/mmol) by the alkylation of the nor-methyl precursor with [11C]CH3I. Synthetic yields are good (40-60% from [11C]methyl iodide, corrected for decay, 20 min synthesis), with the product purified by HPLC. In vivo studies of regional brain distribution in CD-1 mice show uptake and retention of tracer in the cortex, striatum, hypothalamus and thalamus, with the highest levels in the hypothalamus and cortex. Specific binding in the cortex and hypothalamus can be reduced by preadministration of 7 mg/kg i.v. unlabeled nisoxetine. The possible value of [11C]nisoxetine as a PET imaging agent is discussed.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Fluoxetine,
http://linkedlifedata.com/resource/pubmed/chemical/Neurotransmitter Uptake Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/nisoxetine
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pubmed:status |
MEDLINE
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pubmed:issn |
0883-2897
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
771-4
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pubmed:dateRevised |
2008-2-21
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pubmed:meshHeading |
pubmed-meshheading:2533589-Animals,
pubmed-meshheading:2533589-Brain,
pubmed-meshheading:2533589-Carbon Radioisotopes,
pubmed-meshheading:2533589-Fluoxetine,
pubmed-meshheading:2533589-Isotope Labeling,
pubmed-meshheading:2533589-Mice,
pubmed-meshheading:2533589-Neurotransmitter Uptake Inhibitors,
pubmed-meshheading:2533589-Norepinephrine,
pubmed-meshheading:2533589-Tissue Distribution
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pubmed:year |
1989
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pubmed:articleTitle |
Synthesis and regional mouse brain distribution of [11C]nisoxetine, a norepinephrine uptake inhibitor.
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pubmed:affiliation |
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.
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