8-iso prostaglandin a-1

8-iso Prostaglandin A1 (8-iso PGA1) is an isoprostane and a member in a large family of prostanoids of non-cyclooxygenase origin. It occurs as a common minor impurity in most commercial preparations of PGE1. The biological activity of 8-iso PGA1 has not been studied in depth or reported in the literature.

8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of prostaglandins show greatly diminished agonist activity in vitro compared to the parent free acids.

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.

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。