SPECIFIC PROSTAGLANDIN I-2 SYNTHETASE INHIBITOR, 3-HYDROPEROXY-3-METHYL-2-PHENYL-3H-INDOLE

被引：13

作者：

TERASHITA, Z ^{[1
]}

NISHIKAWA, K ^{[1
]}

TERAO, S ^{[1
]}

NAKAGAWA, M ^{[1
]}

HINO, T ^{[1
]}

机构：

[1] CHIBA UNIV,FAC PHARMACEUT SCI,CHIBA 280,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1979年 / 91卷 / 01期

关键词：

D O I：

10.1016/0006-291X(79)90584-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Inhibitory effects of 3-hydroperoxy-3-methyl-2-phenyl-3H-indole(HPI) on prostaglandin endoperoxide synthase(EC 1.14.99.1) and prostaglandin I2(PGI2) synthetase were compared with those of 15-hydroperoxy-5,8,11,13-eicosatetraenoic acid, namely, 15-hydroperoxyarachidonic acid(15-HPAA) and tranylcypromine (TCP). Sheep seminal vesicle microsomes were used as a source of prostaglandin endoperoxide synthase and bovine aortic microsomes as that of PGI2 synthetase. 15-HPAA and HPI inhibited PGI2 synthetase with IC50s of 5 × 10-7 and 3.5 × 10-6 M, respectively, whereas neither compound had effect on prostaglandin endoperoxide synthase at the concentration inhibiting PGI2 synthetase by 90%. TCP was a weak(IC50 = 5 × 10-4M) PGI2 synthetase inhibitor with low specificity. © 1979.

引用

页码：72 / 78

页数：7

共 9 条

[1] INHIBITORS OF THROMBOXANE SYNTHASE IN HUMAN PLATELETS [J].