Resul B, Stjernschantz J, No K, Liljebris C, Selén G, Astin M, Karlsson M, Bito L Z
Kabi Pharmacia AB Ophthalmics, Uppsala, Sweden.
J Med Chem. 1993 Jan 22;36(2):243-8. doi: 10.1021/jm00054a008.
A series of phenyl-substituted analogues of prostaglandin F2 alpha (PGF2 alpha) were prepared and evaluated for ocular hypotensive effect and side effects in different animal models. In addition, the activity of the analogues on FP receptors was studied in vitro. The results were compared with those of PGF2 alpha and its isopropyl ester. The phenyl-substituted PGF2 alpha analogues exhibited good intraocular pressure reducing effect, were more selective, and exhibited a much higher therapeutic index in the eye than PGF2 alpha or its isopropyl ester. The analogues exhibited high activity on FP receptors in a stereoselective manner for the 15 alpha-hydroxyl group.
制备了一系列前列腺素F2α（PGF2α）的苯基取代类似物，并在不同动物模型中评估其降眼压作用和副作用。此外，还在体外研究了这些类似物对FP受体的活性。将结果与PGF2α及其异丙酯的结果进行了比较。苯基取代的PGF2α类似物表现出良好的降低眼压效果，更具选择性，并且在眼中的治疗指数比PGF2α或其异丙酯高得多。这些类似物以立体选择性方式对15α-羟基在FP受体上表现出高活性。
