Minor Structural Modifications Convert the Dual TP/CRTH2 Antagonist Ramatroban into a Highly Selective and Potent CRTH2 Antagonist

Ramatroban, a thromboxane A2 receptor (TP) antagonist with clinical efficacy in asthma and allergic rhinitis, was recently shown to also antagonize the prostaglandin D2 receptor CRTH2. Here we report that minor structural changes to ramatroban result in a compound (13) with complete lack of activity...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 48; no. 4; pp. 897 - 900
Main Authors Ulven, Trond, Kostenis, Evi
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 24.02.2005
Amer Chemical Soc
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Summary:Ramatroban, a thromboxane A2 receptor (TP) antagonist with clinical efficacy in asthma and allergic rhinitis, was recently shown to also antagonize the prostaglandin D2 receptor CRTH2. Here we report that minor structural changes to ramatroban result in a compound (13) with complete lack of activity on TP but sub-nanomolar potency toward CRTH2. This is the first selective CRTH2 antagonist described to date, and should prove highly valuable in further elucidating the biological significance of CRTH2.
Bibliography:ark:/67375/TPS-98LN29GR-B
istex:2BA8FA9153A5A3F3B2C406956F302CC5F43D83F2
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0022-2623
1520-4804
DOI:10.1021/jm049036i