iloprost

Iloprost (Ciloprost) 是前列腺素 I2 的稳定合成类似物，是一种血小板聚集和血管扩张抑制剂，可用于研究心血管疾病。

(Z)-Iloprost ((Z)-Ciloprost; (Z)-ZK 36374) 是一种血管扩张剂，用于预防肝素引起的血小板活化。

15-KetoIloprost是Iloprost的C-15氧化衍生物。Iloprost (ZK 36374) 是前列环素 (PGI2) 的类似物，涉及胚胎发育和改善炎症，并抑制肿瘤转移。

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(R)-Iloprost inhibits platelet aggregation with an IC50 value of 65 nM.

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(S)-Iloprost potently inhibits platelet aggregation with an IC50 value of 3.5 nM.

5-cis-15(R)-Iloprost (5-cis-15(R)-Ciloprost) 是 Iloprost 的 C-5 cis-isomer 和 15(R)-epimer 异构体。Iloprost 是一种前列环素 (PGI2) 类似物，参与胚胎发育、改善炎症，并抑制肿瘤转移。Iloprost 可用于外周血管的研究。

sulotroban 是一种TXA2受体拮抗剂，与伊洛前列素具有协同作用，可抑制TXA2依赖性血小板活化。

CAY10449 是 I 型前列腺素受体 (I prostanoid receptor) 的拮抗剂。它能够逆转伊洛前列素导致的跨上皮电阻 (TEER) 降低，还能逆转ONO-1301 在小鼠模型中的作用。CAY10449 可用于哮喘和过敏性气道炎症研究。

Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-5(Z)-E is a structural analog of 14,15-epoxyeicosatrienoic acids (14,15-EET) that antagonizes EET-induced relaxation of vascular smooth muscle. Relaxation of U46619-constricted bovine arteries by 14,15-EET could be inhibited approximately 80% by 14,15-EE-5(Z)-E at a concentration of 10 μM. 14,15-EE-5(Z)-E does not appear to antagonize nitric oxide- or iloprost-mediated vascular relaxation.

RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。

BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. BMY 42393 competed for radiolabeled iloprost and PGE1 binding to platelet membranes (IC50; 170 nM and 130 nM, respectively).