Discovery and characterization of a potent and selective EP4 receptor antagonist. Issue 16 (15th August 2015) - Schiffler, Matthew A.
Graphical abstract: Abstract: EP4 is a prostaglandin E2 receptor that is a target for potential anti-nociceptive therapy. Described herein is a class of amphoteric EP4 antagonists which reverses PGE2 -induced suppression of TNFα production in human whole blood. From this class, a potent and highly bioavailable compound (6 ) has been selected for potential clinical studies. EP4 binding and functional data, selectivity, and pharmacokinetic properties of this compound are included.