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rdf:type |
|
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lifeskim:mentions |
umls-concept:C0018787,
umls-concept:C0032743,
umls-concept:C0035647,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0439855,
umls-concept:C0521451,
umls-concept:C1522485,
umls-concept:C1883254,
umls-concept:C1999216
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pubmed:issue |
18
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pubmed:dateCreated |
2007-8-30
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|
pubmed:abstractText |
A series of fluorinated chromone analogs with IC50 values ranging from 9 to 133 nM for the mitochondrial complex 1 (MC-I) has been prepared. A structure-activity relationship (SAR) study of the most potent fluorinated chromone analog 10 demonstrated the linkage heteroatom preference of the side chain region of the molecule while maintaining potent MC-I inhibitory activity. Tissue distribution studies 30 min after [(18)F]10 administration to Sprague-Dawley (SD) rats demonstrated high uptake of the radiotracer from the blood pool into the myocardium (2.24% ID/g), kidney (1.93% ID/g), and liver (2.00% ID/g). After 2 h about 66% of the activity in the myocardium at 30 min had been retained, whereas approximately 70% had been cleared from the liver and kidney. MicroPET images of SD rats after [(18)F]10 administration allowed easy assessment of the myocardium through 60 min with minimal lung or liver interference.
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pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Sep
|
|
pubmed:issn |
0022-2623
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|
pubmed:author |
pubmed-author:AzureMichaelM,
pubmed-author:CasebierDavidD,
pubmed-author:GuaraldiMaryM,
pubmed-author:HansonKelleyK,
pubmed-author:HayesMeganM,
pubmed-author:KaganMikhailM,
pubmed-author:RadekeHeikeH,
pubmed-author:RobinsonSimonS,
pubmed-author:YalamanchiliPadmajaP,
pubmed-author:YuMingM,
pubmed-author:ZhangZhi-QinZQ
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|
pubmed:issnType |
Print
|
|
pubmed:day |
6
|
|
pubmed:volume |
50
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
4304-15
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|
pubmed:meshHeading |
pubmed-meshheading:17696417-Animals,
pubmed-meshheading:17696417-Cattle,
pubmed-meshheading:17696417-Chromones,
pubmed-meshheading:17696417-Electron Transport Complex I,
pubmed-meshheading:17696417-Fluorine Radioisotopes,
pubmed-meshheading:17696417-Heart,
pubmed-meshheading:17696417-Isotope Labeling,
pubmed-meshheading:17696417-Kidney,
pubmed-meshheading:17696417-Liver,
pubmed-meshheading:17696417-Lung,
pubmed-meshheading:17696417-Male,
pubmed-meshheading:17696417-Myocardium,
pubmed-meshheading:17696417-Positron-Emission Tomography,
pubmed-meshheading:17696417-Radiopharmaceuticals,
pubmed-meshheading:17696417-Rats,
pubmed-meshheading:17696417-Rats, Sprague-Dawley,
pubmed-meshheading:17696417-Structure-Activity Relationship,
pubmed-meshheading:17696417-Submitochondrial Particles,
pubmed-meshheading:17696417-Sulfides,
pubmed-meshheading:17696417-Technetium Tc 99m Sestamibi,
pubmed-meshheading:17696417-Tissue Distribution
|
|
pubmed:year |
2007
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|
pubmed:articleTitle |
Synthesis and biological evaluation of the mitochondrial complex 1 inhibitor 2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromene-4-one as a potential cardiac positron emission tomography tracer.
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|
pubmed:affiliation |
Research and Development, Bristol-Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA. heike.radeke@bms.com
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pubmed:publicationType |
Journal Article,
In Vitro
|
