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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2007-1-22
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pubmed:abstractText |
Structure-activity relationship (SAR) studies of 3-arylpropionic acids-a class of novel S1P(1) selective agonists-by introducing substitution to the propionic acid chain and replacing the adjacent phenyl ring with pyridine led to a series of modified 3-arylpropionic acids with enhanced half-life in rat. These analogs (e.g., cyclopropanecarboxylic acids) exhibited longer half-life in rat than did unmodified 3-arylpropionic acids. This result suggests that metabolic oxidation at the propionic acid chain, particularly at the C3 benzylic position of 3-arylpropionic acids, is probably responsible for their short half-life in rodent.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BergstromJamesJ,
pubmed-author:CardDeborahD,
pubmed-author:ChrebetGaryG,
pubmed-author:HajduRichardR,
pubmed-author:HaleJeffrey JJJ,
pubmed-author:JkoE SES,
pubmed-author:KeohaneCarol ACA,
pubmed-author:MandalaSuzanne MSM,
pubmed-author:MilliganJames AJA,
pubmed-author:MillsSander GSG,
pubmed-author:OrrV BVB,
pubmed-author:RosenbachMark JMJ,
pubmed-author:SheiGan-JuGJ
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
828-31
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pubmed:meshHeading |
pubmed-meshheading:17092714-Animals,
pubmed-meshheading:17092714-Biological Availability,
pubmed-meshheading:17092714-CHO Cells,
pubmed-meshheading:17092714-Cricetinae,
pubmed-meshheading:17092714-Cricetulus,
pubmed-meshheading:17092714-Guanosine 5'-O-(3-Thiotriphosphate),
pubmed-meshheading:17092714-Half-Life,
pubmed-meshheading:17092714-Lymphocyte Count,
pubmed-meshheading:17092714-Lymphocytes,
pubmed-meshheading:17092714-Male,
pubmed-meshheading:17092714-Mice,
pubmed-meshheading:17092714-Propionic Acids,
pubmed-meshheading:17092714-Rats,
pubmed-meshheading:17092714-Rats, Sprague-Dawley,
pubmed-meshheading:17092714-Receptors, Lysosphingolipid,
pubmed-meshheading:17092714-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. lin_yan@merck.com
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pubmed:publicationType |
Journal Article
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