rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
5
|
pubmed:dateCreated |
2010-3-4
|
pubmed:abstractText |
The discovery of highly potent and selective second generation EP(4) antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
1520-4804
|
pubmed:author |
pubmed-author:BlouinMarcM,
pubmed-author:BurchJasonJ,
pubmed-author:ClarkPatsyP,
pubmed-author:DenisDanielleD,
pubmed-author:DucharmeYvesY,
pubmed-author:FarandJulieJ,
pubmed-author:FriesenRickR,
pubmed-author:GaudreaultMireilleM,
pubmed-author:HanYongxinY,
pubmed-author:LévesqueJean-FrançoisJF,
pubmed-author:MathieuMarie-ClaudeMC,
pubmed-author:MellonChristopheC,
pubmed-author:O'NeillGaryG,
pubmed-author:RowlandSteveS,
pubmed-author:StoccoRinoR,
pubmed-author:TherienAlexA,
pubmed-author:VigneaultErikaE,
pubmed-author:WronaMarkM,
pubmed-author:XuDaigenD
|
pubmed:issnType |
Electronic
|
pubmed:day |
11
|
pubmed:volume |
53
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2227-38
|
pubmed:meshHeading |
pubmed-meshheading:20163116-Analgesics,
pubmed-meshheading:20163116-Animals,
pubmed-meshheading:20163116-Benzoic Acids,
pubmed-meshheading:20163116-Cyclopropanes,
pubmed-meshheading:20163116-Half-Life,
pubmed-meshheading:20163116-Humans,
pubmed-meshheading:20163116-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20163116-Male,
pubmed-meshheading:20163116-Pain,
pubmed-meshheading:20163116-Prostaglandin Antagonists,
pubmed-meshheading:20163116-Rats,
pubmed-meshheading:20163116-Rats, Sprague-Dawley,
pubmed-meshheading:20163116-Receptors, Prostaglandin E,
pubmed-meshheading:20163116-Structure-Activity Relationship,
pubmed-meshheading:20163116-Thiophenes
|
pubmed:year |
2010
|
pubmed:articleTitle |
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada Ltd., 16771 Trans-Canada Highway, Kirkland, QC, Canada. marc_blouin@merck.com
|
pubmed:publicationType |
Journal Article
|