rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
10
|
pubmed:dateCreated |
2008-5-16
|
pubmed:abstractText |
A series of fluorinated pyridazinone derivatives with IC50 values ranging from 8 to 4000 nM for the mitochondrial complex 1 (MC1) have been prepared. Structure-activity relationship (SAR) assessment indicated preference of the fluorine label to be incorporated on an alkyl side chain rather than directly on the pyridazinone moiety. Tissue distribution studies of a series of analogues ([18F] 22-28) in Sprague-Dawley (SD) rats identified [18F]27 as the most promising radiotracer with high uptake in cardiac tissue (3.41%ID/g; 30 min post injection) in addition to favorable heart to nontarget organ distribution ratios. MicroPET images of SD rats and nonhuman primates after [18F]27 administration allowed easy assessment of the myocardium through 60 min with minimal lung or liver interference.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0022-2623
|
pubmed:author |
pubmed-author:AzureMichaelM,
pubmed-author:BenettiRichardR,
pubmed-author:CasebierDavidD,
pubmed-author:GOODA EAE,
pubmed-author:GuaraldiMaryM,
pubmed-author:HansonKelleyK,
pubmed-author:HayesMeganM,
pubmed-author:KaganMikhailM,
pubmed-author:PurohitAjayA,
pubmed-author:RadekeHeikeH,
pubmed-author:RobinsonSimonS,
pubmed-author:YalamanchiliPadmajaP,
pubmed-author:YuMingM
|
pubmed:issnType |
Print
|
pubmed:day |
22
|
pubmed:volume |
51
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2954-70
|
pubmed:meshHeading |
pubmed-meshheading:18422306-Animals,
pubmed-meshheading:18422306-Cattle,
pubmed-meshheading:18422306-Electron Transport Complex I,
pubmed-meshheading:18422306-Female,
pubmed-meshheading:18422306-Fluorine Radioisotopes,
pubmed-meshheading:18422306-Heart,
pubmed-meshheading:18422306-Macaca mulatta,
pubmed-meshheading:18422306-Male,
pubmed-meshheading:18422306-Mitochondria, Heart,
pubmed-meshheading:18422306-Positron-Emission Tomography,
pubmed-meshheading:18422306-Pyridazines,
pubmed-meshheading:18422306-Radiopharmaceuticals,
pubmed-meshheading:18422306-Rats,
pubmed-meshheading:18422306-Rats, Sprague-Dawley,
pubmed-meshheading:18422306-Structure-Activity Relationship,
pubmed-meshheading:18422306-Tissue Distribution
|
pubmed:year |
2008
|
pubmed:articleTitle |
Synthesis and biological evaluation of pyridazinone analogues as potential cardiac positron emission tomography tracers.
|
pubmed:affiliation |
Research and Development, Bristol-Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA.
|
pubmed:publicationType |
Journal Article,
In Vitro
|