前列腺素V（1）。（±）-11-脱氧-10-羟基前列腺素E1甲酯的合成与药理学

Prostaglandins V (1). Synthesis and pharmacology of (+/-)-11-deoxy-10-hydroxyprostaglandin E1 methyl ester.

作者信息

Caton M P, Darnbrough G, Hambling D J, Jordon R, Parker T

出版信息

Prostaglandins. 1979 Oct;18(4):569-76. doi: 10.1016/0090-6980(79)90024-8.

Abstract

(+/-)-Deoxy-10-hydroxy-PGE1 methyl ester (Va) has been synthesised via conjugate addition of the cuprate (III) to the 5-tetrahydropyranyloxycyclopentenone (IId). Va was found to be 0.1 times as active as PGE1 as a uterine stimulant in the anaesthetized pregnant rat, 0.25 times as active as PGE1 in causing vasodepression in the anaesthetized cat, and approximately equiactive to PGE1 in inducing bronchoconstriction.

摘要

（±）-脱氧-10-羟基前列地尔甲酯（Va）是通过将铜酸盐（III）共轭加成到5-四氢吡喃氧基环戊烯酮（IId）上合成的。在麻醉的妊娠大鼠中，Va作为子宫兴奋剂的活性是PGE1的0.1倍；在麻醉的猫中，Va引起血管抑制的活性是PGE1的0.25倍；在诱导支气管收缩方面，Va与PGE1的活性大致相当。