ONO-8130 is an orally bioavailable and selective antagonist of the prostaglandin E2 (PGE2) receptor EP1 with Ki value of 1.9 nM.
Prostaglandins contribute to the sensitization of peripheral and central nociceptive neurons during peripheral inflammation. Prostaglandin E2 (PGE2) is considered a dominant pronociceptive prostanoid. PGE2 receptors are G protein-coupled receptors and classified into 4 general subtypes (EP1, EP2, EP3, and EP4) that are located unevenly in different tissues. EP1 receptors play a major role in processing of pain.