tp receptor

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。

TP receptor antagonist-1 (compound 7m) 作为血栓素 A2受体 (TP 受体) 的拮抗剂，其对TPa 和 TPb 的IC50值分别为 9.46 μM 和 8.49 μM。该化合物常用于心血管疾病的研究领域。

TP receptor antagonist-2 (example 7n) 为血栓素 A2受体 (TP 受体) 的拮抗剂，其对TPα和TPβ的IC50值分别为5.64 μM 和5.27 μM。此化合物具有抑制血小板聚集的功能。

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

Treprostinil (Orenitram) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。

Treprostinil Sodium (UT-15) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。

Prostaglandin J2 (PGJ2) 是前列腺素 D2 (PGD2) 的一种内源性代谢物，是一种有效的 PGD2 受体 (DP) 激动剂，对 hDP 和 hCRTH2 的 Ki 分别为 0.9 nM 和 6.6 nM。Prostaglandin J2 刺激细胞内环 AMP 的产生，EC50值为 1.2 nM。Prostaglandin J2 诱导氧化应激和神经细胞凋亡。Prostaglandin J2 诱导泛素化 (Ub) 蛋白的积累 聚集。Prostaglandin J2 具有高度神经毒性，可导致许多神经退行性疾病，包括阿尔茨海默病 (AD) 和帕金森病 (PD)。

Thymopentin (TP5) 是主要由胸腺皮质和髓质上皮细胞分泌的生物特性肽。它能促使自人类胚胎干细胞产生 T 细胞群。它是有效免疫调节剂，具有很短的血浆半衰期(30 秒)。

Seratrodast (ABT-001) 是一种血栓素 A2 受体 (TP) 拮抗剂，用于治疗哮喘。

KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.

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).

GW627368 (GW 627368X) 是一种新型、强效和选择性的前列腺素 EP4 受体拮抗剂，还对血栓素受体TP 有亲和力。对人 EP4 和 TP 的pKi 值分别为 7.0 和 6.8。

Dubermatinib (TP0903) 是一种具有高效性和选择性的 Axl 受体酪氨酸激酶抑制剂，IC50值为27 nM。

TP003是一种新型的非选择性GABAA 受体苯二氮卓位点激动剂，对α1β2γ2、α2β3γ2、α3β3γ2、α5β2γ2 的具有亲和力，其EC50 分别20.3、10.6、3.24、5.64 nM。 TP003 通过 α2GABAA 受体从而具有抗焦虑活性，也有部分抗惊厥活性。

RS 61756-007 is a selective thromboxane receptor (TP) agonist.

ICI 192605 is a potent thromboxane A2 receptor (TP receptor) antagonist.

R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold

TP-680 is a antagonist of cholecystokininA receptor.

I-BOP 是血栓素 A2 受体 (TP) 的激动剂（KD=0.61 nM）。I-BOP 可通过激活血管平滑肌中的 PI3K 通路促进细胞增殖。

I-SAP is a high affinity TP receptor antagonist. At physiologic pH, I-SAP produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM. I-SAP binds to human platelets with the maximum binding obtained between pH 6.5 and pH 7.4. In washed human platelets, the Kd for I-SAP is 468 pM at pH 7.4 and 490 pM at pH 6.5.

8-iso PGF3α is an isoprostane produced from the free-radical peroxidation of EPA. Little is known about the biological activity of 8-iso PGF3α. There is one report that it is inactive in a TP receptor mediated assay of human platelet shape change, where 8-iso PGF2α has an ED50 value of 1 uM. [1]

8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-isoprostane (8-iso PGF2α) is a prostaglandin-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-iso PGF2α is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-iso PGF2α is infused into rabbits. Early in the infusion (within 1-2 minutes) 8-iso -15-keto PGF2α was a major component of the metabolite profile, which was comprised mostly of unmetabolized 8-iso PGF2α. 8-iso -15-keto PGF2α is a vasoconstrictor when tested on the rat isolated thoracic aorta, acting via the TP (thromboxane) receptor.

TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.

12(S)-HETE 是花生四烯酸的12-脂氧合酶代谢产物，对癌细胞增殖具有促有丝分裂作用，可增强血管紧张素 II 诱导的 BLT2 收缩（白三烯 B4小鼠动脉中 2 型受体）和 TP （血栓素受体） 介导的机制。12(S)-HETE促进动脉内皮细胞中超氧化物和异血栓素样代谢物的产生。