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 (DP1, EP2), 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
2062 Alprostadil Prostaglandin EP (1-4) receptor antagonist €125.00
2145 AZD1981 Selective CRTH2 (aka DP2) antagonist €90.00
3073 BAY 1316957 Highly potent, specific, and selective PGE2 receptor hEP4 antagonist €150.00
2788 ER-819762 Highly selective, and orally available PGE2 receptor EP4 antagonist €155.00
3787 Grapiprant Potent, selective, competitive and orally bioavailable prostaglandin EP4 receptor antagonist €100.00
1210 ICI 192605 Thromboxane A2 antagonist €120.00
1480 MK 0524 sodium salt PGD2 receptor DP1 antagonist €130.00
1512 ONO 8711 dicyclohexyl amine salt PGE1 receptor EP1 antagonist €120.00
2024 PF 04418948 Prostaglandin EP2 receptor antagonist €95.00
2874 Ralinepag Potent, orally active IP receptor (PGI2) agonist €150.00
1605 S 5751 PGD2 receptor DP1 antagonist €115.00
2605 Selexipag Prodrug of MRE 269, a potent IP receptor (PGI2) agonist €90.00
1447 Seratrodast Thromboxane A2 antagonist €85.00
3212 TG11-77 hydrochloride Potent, selective, water soluble, brain-permeable EP2 receptor antagonist €130.00
1913 Timapiprant Selective DP2 (CRTH2) antagonist €90.00
3966 TM30089 sodium Selective CRTH2 antagonist Inquire

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