prostaglandin f1α

Prostaglandin F1α(PGF1α)是一种脂质介质和prostacyclin的内源性代谢物，主要由DGLA经过COX途径代谢生成，能够剂量依赖性地调节平滑肌收缩。

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.

6,15-diketo-13,14-dihydro PGF1α is a metabolite of PGI2. It was shown to enhance intracellular cAMP and cholesterol catabolism in bovine arterial smooth muscle cells.

11-deoxy PGF1α is a synthetic analog of PGF1α. In whole animal studies, a dose of 32 mg kg inhibited gastric acid secretion by 35%. 11-deoxy PGF1α is also known to cause rat uterine contractions at a dose 0.3 times that of PGF1α. It also exhibits vasopressor and bronchoconstrictor activities at about half the potency of PGF2α in guinea pigs.

15-keto PGF1α is the initial metabolite of PGF1α via 15-hydroxy PGDH. In mammals, oxidation of C-15 markedly attenuates receptor binding and activity. In fish, the 15-keto compounds serve as post-ovulatory pheromones and are more active than the parent prostaglandins.

2,3-dinor-8-iso Prostaglandin F1α（2,3-dinor-8-iso PGF1α）是一种异前列腺素和花生四烯酸的活性代谢物，也是血小板聚集抑制剂8-iso PGF2α的产物。它通过花生四烯酸的非酶促自由基过氧化作用形成。2,3-dinor-8-iso PGF1α在孤立的猪视网膜和大脑微血管中引起血管收缩（EC50s分别为12.8和18.5 nM），但在31 µM的浓度下使用时不会引起孤立的大鼠主动脉环的收缩。在1 µM的浓度下使用时，它能增加孤立的猪大脑切片中的血栓素B2（TXB2）水平，这一效应可以通过血栓素A合成酶抑制剂CGS 12970、电压门控钙通道抑制剂SKF 96365或烟碱型乙酰胆碱受体（nAChR）拮抗剂α-conotoxin来逆转。

Δ17-6-keto Prostaglandin F1α (Δ17-6-keto PGF1α), a cyclooxygenase (COX) metabolite produced from eicosapentaenoic acid (EPA) in a variety of tissues including seminal vesicles, lungs, polymorphonuclear leukocytes, and ocular tissues, alongside other 3-series COX products from EPA such as PGF3α, PGE3, and thromboxane B3, is potentially linked to a lower occurrence of glaucoma in individuals consuming a marine-rich (EPA-rich) diet.

PGF1β, a biochemical compound, functions as a pivotal mediator in inflammatory processes and plays an integral role in uterine contractions. It exhibits significant regulatory effects on platelet aggregation and vasodilation, demonstrating its critical importance in cardiovascular health. Additionally, PGF1β contributes to the regulation of kidney function and electrolyte balance, illustrating its widespread impact across various physiological systems.

11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 μg kg.

8-iso Prostaglandin F1α（8-异前列腺素 F1α）是一种由花生四烯酸产生的异前列腺素，能引起浓度依赖性的的血管收缩效应，包括肺动脉（PA）、肺静脉（PV）和肠系膜动脉（MA），通过TXA2R、酪氨酸激酶和Rho激酶的激活。

17-TFM-PGF1α (Compound 8) 为一种饱和前列腺素类似物。此化合物对人前列腺素 F 受体 (hFP receptor) 表现出较强的亲和性和受体选择性，其EC50为 85 nM。

8-iso Prostaglandin F1β（8-异前列腺素 F1β）是一种由花生四烯酸产生的异前列腺素，能引起浓度依赖性的的血管收缩效应，包括肺动脉（PA）、肺静脉（PV）和肠系膜动脉（MA），通过TXA2R、酪氨酸激酶和Rho激酶的激活。

1-Methylnicotinamide是nicotinamide的活性代谢产物，由nicotinamide N-methyltransferase催化形成。1-Methylnicotinamide以浓度依赖的方式诱导人脐静脉内皮细胞（HUVECs）分泌一氧化氮。当以30 mg/kg剂量给药时，能增加大鼠血浆6-keto-prostaglandin F1α水平，并在相同剂量下抑制大鼠胶原诱导的血栓形成。

Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously express COX-2. Lornoxicam reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays with IC50 values of 65 and 54 µM, respectively. It reduces carrageenan-induced paw edema in rats when administered intravenously at doses ranging from 0.1 to 9 mg kg. Formulations containing lornoxicam have been used in the management of postoperative pain.

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1 BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.

9-Keto Fluprostenol Isopropyl Ester, an ester derivative of the FP receptor agonist fluprostenol, undergoes oxidation at carbon 9. This compound serves as a potential prodrug for 9-keto fluprostenol, which may function as an agonist at EP receptors. Additionally, it is considered a possible metabolite of fluprostenol isopropyl ester (travoprost), drawing parallels to the metabolism of latanoprost by 15-hydroxyprostaglandin dehydrogenase observed in monkey cornea. Furthermore, certain F-series prostaglandins, such as 6-keto prostaglandin F1α (PGF1α), undergo conversion to their E-series counterparts in isolated human platelets, highlighting a metabolic pathway of relevance.