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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1997-6-19
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pubmed:abstractText |
No-carrier-added (NCA)[11C](+/-)-ketamine (2a) and its enantiomers (+)-2b and (-)-2c were synthesized by methylation of the corresponding norketamine (1a-c) with [11C]H3I in an overall radiochemical yield of 20% (EOB) with specific activities of 0.35-0.45 Ci/mumol at EOB in a synthesis time of 40 min from EOB. Compound 2a was metabolized rapidly in mouse brain and labeled metabolites appeared in baboon plasma. PET studies of compounds 2a-c in a baboon showed that influx of compounds 2a-c into the brain was high for the first few min but radioactivity then declined rapidly. Although the retention of radioactivity in the baboon striatum was not significantly different for 2a-c 20 min post-injection, graphical analysis of time-activity data for each enantiomer and for the racemate in baboon striatum suggested that (+)-ketamine may interact with receptors slightly more effectively than its (-)-enantiomer or racemate. However, due to its rapid metabolism in the brain and a similar uptake in the striatum and cerebellum, [11C]ketamine may not be an ideal tracer for studying NMDA receptor with PET.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
|
pubmed:issn |
0969-8051
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
24
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
145-50
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:9089707-Animals,
pubmed-meshheading:9089707-Biological Transport,
pubmed-meshheading:9089707-Biotransformation,
pubmed-meshheading:9089707-Brain,
pubmed-meshheading:9089707-Carbon Radioisotopes,
pubmed-meshheading:9089707-Female,
pubmed-meshheading:9089707-Isotope Labeling,
pubmed-meshheading:9089707-Ketamine,
pubmed-meshheading:9089707-Mice,
pubmed-meshheading:9089707-Mice, Inbred Strains,
pubmed-meshheading:9089707-Papio,
pubmed-meshheading:9089707-Tissue Distribution,
pubmed-meshheading:9089707-Tomography, Emission-Computed
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pubmed:year |
1997
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pubmed:articleTitle |
Carbon-11 labelled ketamine-synthesis, distribution in mice and PET studies in baboons.
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pubmed:affiliation |
Chemistry Department, Brookhaven National Laboratory, Upton, New York 11973, USA.
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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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