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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
26
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pubmed:dateCreated |
2005-12-21
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pubmed:abstractText |
Ring-constrained adenosine analogues have been designed to act as dual agonists at tissue-protective A(1) and A(3) adenosine receptors (ARs). 9-Ribosides transformed into the ring-constrained (N)-methanocarba-2-chloro-5'-uronamides consistently lost affinity at A(1)/A(2A)ARs and gained at A(3)AR. Among 9-riboside derivatives, only N(6)-cyclopentyl and 7-norbornyl moieties were extrapolated for mixed A(1)/A(3) selectivity and rat/human A(3)AR equipotency. Consequently, 2 was balanced in affinity and potency at A(1)/A(3)ARs as envisioned and dramatically protected in an intact heart model of global ischemia and reperfusion.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-10225368,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-10877835,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-10887176,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-11605996,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-11734617,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-11743234,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-11784146,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12234780,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12234810,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12238926,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12500024,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12754103,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12793983,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-12919933,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15080906,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15602551,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15651784,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15681707,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15743197,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15771421,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-15797469,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-7954592,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-8022403,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-9415272,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-9618527,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16366590-9703463
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine A1 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine A2 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine A3 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Cardiotonic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A2A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Adenosine A3
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8103-7
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:16366590-Adenosine,
pubmed-meshheading:16366590-Adenosine A1 Receptor Agonists,
pubmed-meshheading:16366590-Adenosine A2 Receptor Agonists,
pubmed-meshheading:16366590-Adenosine A3 Receptor Agonists,
pubmed-meshheading:16366590-Animals,
pubmed-meshheading:16366590-CHO Cells,
pubmed-meshheading:16366590-Cardiotonic Agents,
pubmed-meshheading:16366590-Cricetinae,
pubmed-meshheading:16366590-Drug Design,
pubmed-meshheading:16366590-Humans,
pubmed-meshheading:16366590-Mice,
pubmed-meshheading:16366590-Myocardial Infarction,
pubmed-meshheading:16366590-Receptor, Adenosine A1,
pubmed-meshheading:16366590-Receptor, Adenosine A2A,
pubmed-meshheading:16366590-Receptor, Adenosine A3,
pubmed-meshheading:16366590-Reperfusion Injury,
pubmed-meshheading:16366590-Ventricular Function, Left
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pubmed:year |
2005
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pubmed:articleTitle |
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
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pubmed:affiliation |
National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA. kajacobs@helix.nih.gov
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural,
Research Support, N.I.H., Intramural
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