Literature DB >> 12643927

Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.

Xavier Billot1, Anne Chateauneuf, Nathalie Chauret, Danielle Denis, Gillian Greig, Marie Claude Mathieu, Kathleen M Metters, Deborah M Slipetz, Robert N Young.   

Abstract

Analogues of PGE(2) wherein the hydroxycyclopentanone ring has been replaced by a lactam have been prepared and evaluated as ligands for the EP(4) receptor. An optimized compound (19a) shows high potency and agonist efficacy at the EP(4) receptor and is highly selective over the other seven known prostaglandin receptors.

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Year:  2003        PMID： 12643927     DOI： 10.1016/s0960-894x(03)00042-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  24 in total

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5.  Lubiprostone targets prostanoid EP₄ receptors in ovine airways.

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Journal:  Br J Pharmacol       Date:  2011-01       Impact factor: 8.739

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Review 7.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

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Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

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10.  Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype.

Authors:  N Foudi; L Kotelevets; L Louedec; G Leséche; D Henin; E Chastre; X Norel
Journal:  Br J Pharmacol       Date:  2008-06-02       Impact factor: 8.739
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