Source:http://linkedlifedata.com/resource/pubmed/id/16253808
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
8
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| pubmed:dateCreated |
2005-10-28
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| pubmed:abstractText |
This report describes the synthesis of [11C]2-(1-methyl-4-piperidinyl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-3(2H)-pyridazinone ([11C]FR194921), a highly selective, nonxanthine-type adenosine A(1) receptor antagonist, used in brain imaging in rats and conscious monkeys as a potential novel PET tracer. [11C]FR194921 was successfully synthesized in 19 min after [11C]CH3I formation. The radiochemical yield was 38+/-3%; and radioactivity was 4.1+/-0.4 GBq, calculated from end of synthesis; radiochemical purity was higher than 99%; and the specific radioactivity was 25.0+/-8.1 GBq micromol(-1) (n=5). In a rat experiment, the distribution of [11C]FR194921 was higher in the hippocampus, striatum and cerebellum regions. This accumulation was significantly decreased by approximately 50% by pretreatment with 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), an adenosine A1 receptor antagonist, which indicated specific binding of the radioligand to adenosine A1 receptors. In conscious monkey PET experiments, [11C]FR194921 accumulated in several regions of the brain, especially in the occipital cortex, thalamus and striatum. These results suggest that [11C]FR194921 can be used as an agent for imaging adenosine A1 receptors in vivo by positron emission tomography (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/2-(1-methyl-4-piperidinyl)-6-(2-phen...,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine A1 Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A1,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthine
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| pubmed:status |
MEDLINE
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| pubmed:month |
Nov
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| pubmed:issn |
0969-8051
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
32
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
837-44
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:16253808-Adenosine A1 Receptor Antagonists,
pubmed-meshheading:16253808-Animals,
pubmed-meshheading:16253808-Brain,
pubmed-meshheading:16253808-Carbon Radioisotopes,
pubmed-meshheading:16253808-Male,
pubmed-meshheading:16253808-Metabolic Clearance Rate,
pubmed-meshheading:16253808-Organ Specificity,
pubmed-meshheading:16253808-Piperidines,
pubmed-meshheading:16253808-Positron-Emission Tomography,
pubmed-meshheading:16253808-Pyridazines,
pubmed-meshheading:16253808-Radiopharmaceuticals,
pubmed-meshheading:16253808-Rats,
pubmed-meshheading:16253808-Rats, Sprague-Dawley,
pubmed-meshheading:16253808-Receptor, Adenosine A1,
pubmed-meshheading:16253808-Staining and Labeling,
pubmed-meshheading:16253808-Tissue Distribution,
pubmed-meshheading:16253808-Whole Body Imaging,
pubmed-meshheading:16253808-Xanthine
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| pubmed:year |
2005
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| pubmed:articleTitle |
Synthesis and evaluation of [11C]FR194921 as a nonxanthine-type PET tracer for adenosine A1 receptors in the brain.
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| pubmed:affiliation |
Basic Research Division, The Medical and Pharmacological Research Center Foundation, Ishikawa 925-0613, Japan. matsuya@mprcf.or.jp
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| pubmed:publicationType |
Journal Article,
Evaluation Studies
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