PGE2 (EP4)

Prostanoids are a subclass of eicosanoids consisting of the prostaglandins, the thromboxanes, and the prostacyclins. They are the cyclooxygenase metabolites of arachidonic acid, and include prostaglandin (PG) D2, PGE2, PGF2α, PGI2, and thromboxane A2[1]. Their activities are related to a diversity of endogenous processes such as inflammation, platelet aggregation, and vasoconstriction/relaxation. Prostanoid receptors belong to the subfamily of GPCR-A14, and can be grouped into three categories, based on the type of heterotrimeric G-protein activated by the different receptors, and thus the cellular response evoked (Gs (DP1EP2), Gq (EP1), and Gi (EP3)).
Prostaglandin D2 (PGD2) is an acidic lipid mediator that is derived from arachidonic acid by the sequential action of cyclooxygenase(s) (COX) and PGD2 synthase(s). Arachidonic acid is converted by COX-1 and COX-2 in a two-step process to first PGG2 and then PGH2. These unstable endoperoxide intermediates are converted to PGD2 by either the haematopoietic or lipocalin PGD2 synthase. PGD2 is produced in the brain where it might be involved in the regulation of sleep and other central nervous system (CNS) activities, including pain perception. In peripheral tissues, the richest cellular source of PGD2 is the mast cell[2].

[1] Prostanoid Receptors: Structures, Properties, and Functions.S Narumiya, Y Sugimoto, F Ushikubi. Physiol Rev 1999, 79, 1193-1226.
[2] R. Pettipher et al. Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases. Nat. Rev. Drug Discov. 2007, 6, 313-325.

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Axon ID Name Description From price
2788 ER-819762 Highly selective, and orally available PGE2 receptor EP4 antagonist €155.00
3073 BAY 1316957 Highly potent, specific, and selective PGE2 receptor hEP4 antagonist €150.00
2062 Alprostadil Prostaglandin EP (1-4) receptor antagonist €125.00

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