dp2

Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂，Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合，Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药，用于治疗性欲减退症。

Timapiprant (OC000459) 是一种有效的选择性 D 前列腺素受体 2(DP2) 拮抗剂，IC50为 13 nM。它抑制肥大细胞激活 Th2 淋巴细胞和嗜酸性粒细胞，有效地置换来自人重组 DP2、大鼠重组 DP2 和人天然 DP2 的 [3H] PGD2。

Dp2mT is an iron chelator which inhibits HIV-1 transcription.

AMG-009 是一种具有选择性和高效性的 CRTH2 和 DP 双重拮抗剂，对 CRTH2 的 IC50 值为 3 nM ，对 DP 受体的 IC50 值为 12 nM。

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂，对哮喘有研究潜力，对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。

Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra

AZD1981 是一种有效且特异性的 CRTh2 (DP2) 受体拮抗剂，IC50为 4 nM，用于研究哮喘、绝经后、药代动力学、哮喘患者和药物相互作用等治疗和基础科学的试验。

CAY10471 Racemate (TM30089 Racemate) 是一种高选择性的 CRTH2 DP 2 受体拮抗剂，对 hCRTH2 的Ki 值为 0.6 nM，对其选择性远高于人血栓素 A2 受体 TP 或 PGD2 受体 DP。它对大小鼠的同源 CRTH2 也具有拮抗作用。

CAY10595 是 CRTh2 (DP2) 受体的拮抗剂，Ki 为 10 nM。

Ramatroban (BAY u3405) 是一种血栓素 A(2) (TxA(2)) 拮抗剂，IC50为 14 nM。它还通过抑制PGD2结合从而拮抗CRTH2，IC50为113 nM。它用于治疗过敏性鼻炎，可用于治疗哮喘的研究。

Fevipiprant (NVP-QAW039) 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂，KD 值为1.1 nM，IC50为0.44 nM，能够引发人体嗜酸性粒细胞的形状变化。

ADP-2341 is a soluble analog of FiVe1.

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.

LAS191859 is a CRTH2 DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2 DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasti

Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2 DP2) with 5-10 fold lower affinity than PGD2.

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.

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-461 sodium is the sodium salt of AM-461 --- a novel DP2 receptor antagonist

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.

AM-461 is a DP2 receptor antagonist.

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。