Prostaglandin F2α methyl ester

PGF2α甲酯是PGF2α的类似物，其中C-1羧基已被酯化为甲酯。PGF2α甲酯是首批显示具有降眼压活性的PG酯之一。该化合物继续成为评估其他降眼压PG前体药物的标准。甲酯的效力比游离酸PGF2α强4-5倍。这种差异归因于角膜渗透性改善，以及酯形式化合物在眼组织中长时间滞留的蓄积效应。将2.5µg剂量的PGF2α-OMe涂抹在猫眼上可使眼压降低6-8mmHg。PGF2α methyl ester is an analog of PGF2α in which the C-1 carboxyl group has been esterified as the methyl ester. PGF2α methyl ester was one of the first PG esters shown to have ocular hypotensive activity. This compound continues to be a standard by which other ocular hypotensive PG prodrugs are evaluated. The methyl ester is about 4-5 times more potent than the free acid, PGF2α. This difference is attributed to improved corneal penetration, and a depot effect of prolonged retention of the ester form of the compound in ocular tissue. A 2.5 µg dose of PGF2α-OMe applied to the eyes of cats results in a 6-8 mm Hg reduction in IOP.