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

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Billot X, Chateauneuf A, Chauret N, Denis D, Greig G, Mathieu MC, Metters KM, Slipetz DM, Young RN

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

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1129-32.

PubMed ID

12643927 [ View in PubMed

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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Analogues of PGE(2) wherein the hydroxycyclopentanone ring has been replaced by a lactam have been prepared and evaluated as ligands for the EP(4) receptor.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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dinoprostone	Prostaglandin E2 receptor EP4 subtype	IC 50 (nM)	0.7	N/A	N/A	Details
Dinoprostone	Prostaglandin E2 receptor EP4 subtype	EC 50 (nM)	3	N/A	N/A	Details