prostaglandin d2 receptor

Nedocromil (FPL 59002) 对多种介质的作用或形成有抑制作用，包括组胺，前列腺素 D2和白三烯 C4。

AM211 (AM211 free acid) 是可口服的选择性前列腺素受体拮抗剂，对人、小鼠、豚鼠和大鼠的 DP2 的IC50值分别为 4.9、7.8、4.9 和 10.4 nM。

PGD2-IN-1 (PGD2-inhibitor) 是 一种有效的DP 受体拮抗剂(IC50 : 0.3 nM),是一种可以抑制前列腺素D2 (PGD2)信号传导的化合物。PGD2-IN-1 专门针对和调节PGD2受体或参与PGD2合成或代谢的酶的活性。

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂，Ki 为 0.57 nM，对 TP 受体的 Ki 为 2.95 nM。

L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively).

O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981) 2.Morgan, A.G.M., Babu, D., Michail, K., et al.An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivityToxicol. Lett.28048-56(2017) 3.Torisu, K., Kobayashi, K., Iwahashi, M., et al.Discovery of new chemical leads for prostaglandin D2 receptor antagonistsBioorg. Med. Chem. Lett.14(17)4557-4562(2004)

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2 DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.

Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of miniature inhibitory postsynaptic currents in primary cultured hippocampal neurons, an effect which is the opposite of that induced by anandamide.. PGD2-EA also induces apoptosis in colorectal carcinoma cell lines.

Pexopiprant, a potent oral antagonist of the prostaglandin D2 receptor 2 (DP2) with a K i value less than 100nM, is a valuable compound for asthma research.

AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay.

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2 DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.

15-deoxy-Δ12,14-Prostaglandin D2 (15-deoxy-Δ12,14-PGD2) is a PGD2 metabolite functioning as an agonist for the PGD2 receptor 2 (DP2), with a binding affinity (Ki) of 50 nM for the mouse DP2 receptor expressed in HEK293 cell membranes. It activates eosinophils with an EC50 of 8 nM and enhances the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), initiating PPARγ-mediated transcription at 5 µM concentration. Furthermore, it exhibits cytotoxicity towards L1210 murine leukemia cells with an IC50 of 0.3 µg ml and displays weaker inhibition of ADP-induced platelet aggregation than PGD2, with an IC50 of 320 ng ml.

15(R)-Prostaglandin D2作为一种潜在的前列腺素DP(2)受体激动剂，展现出抗炎活性。它能促进人嗜酸性粒细胞内肌动蛋白的聚合，同时提高血小板中的cAMP水平。

13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2), a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway, is a selective agonist for the DP2 receptor and can inhibit ion flux in canine colonic mucosa preparation [1].