Source:http://linkedlifedata.com/resource/pubmed/id/20004578
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative library synthesis approach delivered the first selective M(5) PAM (no activity at M(1)-M(4) @ 30microM), and an important tool compound to study the role of M(5) in the CNS.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
558-62
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pubmed:dateRevised |
2011-9-26
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pubmed:meshHeading |
pubmed-meshheading:20004578-Allosteric Regulation,
pubmed-meshheading:20004578-Animals,
pubmed-meshheading:20004578-CHO Cells,
pubmed-meshheading:20004578-Cricetinae,
pubmed-meshheading:20004578-Cricetulus,
pubmed-meshheading:20004578-Drug Design,
pubmed-meshheading:20004578-High-Throughput Screening Assays,
pubmed-meshheading:20004578-Mice,
pubmed-meshheading:20004578-Mice, Knockout,
pubmed-meshheading:20004578-Receptor, Muscarinic M1,
pubmed-meshheading:20004578-Receptor, Muscarinic M3,
pubmed-meshheading:20004578-Receptor, Muscarinic M5,
pubmed-meshheading:20004578-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.
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pubmed:affiliation |
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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