h-ep4

Omidenepag (UR-7276) is a selective and potent prostaglandin E2 receptor 2 (EP2) agonist and a novel topical ocular hypotensive agent.Omidenepag is used in the study of glaucoma and hypertension.

L-644,698 is a selective agonist of human prostanoid DP receptor.

ASP7657 is a novel, potent, and selective prostaglandin EP4 receptor antagonist.

Prostaglandin J2 (PGJ2), a derivative of Prostaglandin D2 (PGD2), serves as a potent agonist for PGD2 receptors (DP), exhibiting affinity constants (K i) of 0.9 nM and 6.6 nM for hDP and hCRTH2 receptors, respectively. It activates cyclic AMP production with an EC50 of 1.2 nM, induces oxidative stress, neuronal apoptosis, and promotes the accumulation of ubiquitinated (Ub) proteins. Notably, PGJ2's neurotoxic properties are implicated in the progression of neurodegenerative diseases such as Alzheimer's (AD) and Parkinson's (PD) [1] [2] [3] [4].

(R)-Vorbipiprant ((R)-CR6086) is an orally effective antagonist of the prostaglandin E2 receptor 4 (EP4), demonstrating a Ki of 16.6 nM for human EP4. It inhibits the production of cAMP induced by PGE2, with an IC50 of 22 nM. Additionally, (R)-Vorbipiprant exhibits immunomodulatory and antiangiogenic activities, having shown potential to alleviate collagen-induced arthritis in mice.

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.