prostaglandin

Phenylbutazone (Butazolidine) 是是非甾体类抗炎药，前列腺素 H 合酶过氧化物酶的还原辅助因子，可诱导肌肉盲样蛋白 1 表达，有用于强直性脊柱炎的研究潜力。

FPL 62064 是 5-脂氧合酶和COX 双重抑制剂，具有抗炎活性，对 RBL-1 胞质 5-脂氧合酶和前列腺素合成酶 (环氧化酶) 的IC50值分别为 3.5 和 3.1 μM。

Pranoprofen (Pyranoprofen) 可抑制COX1 2酶，阻断花生四烯酸转化为二十烷醇，减少前列腺素的合成。它是一种用于眼科的非甾体抗炎试剂。

Tranilast (SB 252218) 是一种抗过敏药物，可抑制炎症细胞释放脂质介质和细胞因子，抑制前列腺素 D2 (PGD2)产生，IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用，具有抗炎和免疫调节作用。

AT56 是口服有活性的脂钙蛋白型前列腺素 D 合酶 (L-PGDS) 选择性抑制剂，其IC50=95 μM，Ki=75 μM。它能够特异性地抑制L-PGDS 催化的 PGD2介导的嗜睡或疼痛反应。

Saralasin acetate(34273-10-4 free base) 是一种非选择性血管紧张素 II 拮抗剂。

SW033291 是有效的15-PGDH 抑制剂，与15-PGDH 亲和力高，Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。

ONO-RS-082 是磷脂酶 A 抑制剂。它抑制PLA2的IC50值为1.0 μM，但即使浓度达到 100 μM 也不抑制 PLC。

16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2 EP4 and has an interaction with the Wnt pathway.

Prostaglandin K1 (compound 46) 是结构修饰的前列环素 (prostanoid) 类似物，针对EP1的EC50和Ki均为2800 nM。

15-deoxy-Δ-12,14-Prostaglandin J2 is a PPARγ agonist.

Bimatoprost is the Allergan trade name for 17-phenyl trinor prostaglandin F2α ethyl amide (17-phenyl trinor PGF2α ethyl amide), an F-series PG analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group produces 15-keto-17-phenyl trinor PGF2α ethyl amide. 15-keto-17-phenyl trinor PGF2α ethyl amide is a potential metabolite of 17-phenyl trinor PGF2α ethyl amide when 17-phenyl trinor PGF2α ethyl amide is administered to intact animals. No pharmacological studies on 15-keto-17-phenyl trinor PGF2α ethyl amide have been reported.

Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood platelet aggregation inhibition assay.

Enzymatically-derived prostaglandin E2 (PGE2) is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings of oxidative stress via the isoprostane pathway. A proposed mechanism for the formation of rac-PGE2 involves the base catalyzed equilibration from 15-E2t-isoprostane (8-iso-PGE2), generated from the 15-H2t-isoprostane endoperoxide.

ent-Prostaglandin F2α 是 PGF2α 的对映体，在尿液中可被发现。

16,16-dimethyl Prostaglandin A1 是一种前列腺素类似物，可以抑制 Lewis 肺癌和 B 16无黑色素瘤细胞中的 DNA 合成 (DNA synthesis)，以及抑制 HSV 和 HIV-1的病毒复制。

16,16-dimethyl PGA2 is a metabolism-resistant analog of PGA2 with a prolonged in vivo half-life. It inhibits the proliferation of Sendai virus in cultured African green monkey kidney cells by >90% at a concentration of 4 μg ml. Daily infusion of 10 μg of 16,16-dimethyl PGA2 methyl ester into mice infected with influenza A virus increased survival by 40%. Similar treatment of mice inoculated with erythroleukemia cells delayed tumor growth and increased survival time.

1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid first identified in extracts of sheep vesicular gland microsomes, known to contain COX, incubated with adrenic acid . 1a,1b-dihomo PGE2 has also been identified in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid . This product is thought to be produced by elongation of AA to adrenic acid, which is then metabolized sequentially by COX and PGE synthase.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM.[1] 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2.2 11β-PGE2 inhibits PGE2 binding to the prostaglandin transporter protein with a Ki of 56 nM.[3] .

13,14-dihydro Prostaglandin F2α (13,14-dihydro PGF2α) is the analog of PGF2α which has no unsaturation in the lower side chain. It causes luteolysis in hamsters with a potency five times higher than PGF2α. The ED50 value for 13,14-dihydro PGF2α as a luteolytic agent in hamsters is 1.5 µg 100 g.[1]

13,14-dihydro-15-keto Prostaglandin E1 可抑制 ADP 诱导的人离体富血小板血浆中的血小板聚集（IC50=14.8 μg mL），也是 PGE1 代谢物。

13,14-dihydro-15-keto Prostaglandin F1α (13,14-dihydro-15-keto PGF1α) is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.

15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2 . In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitory activity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).

15(S)-15-methyl PGE2 is a potent, metabolically stable analog of PGE2. It is a potent gastric antisecretory and antiulcer compound. 15(S)-15-methyl PGE2 binds to human myometrium with twice the affinity of PGE2 and is ten times more potent than PGE1 in contracting uterine smooth muscle.