Inhibitory effects of ethaverine, a homologue of papaverine, on monoamine oxidase activity in mouse brain

被引：8

作者：

Lee, SS

Lee, JJ

Cheong, MJ

Kim, YH

Kim, Y

Yun, YP

Lee, CK

Lee, MK

机构：

[1] Chungbuk Natl Univ, Coll Pharm, Heungduk Ku 361763, Cheongju, South Korea

[2] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea

来源：

BIOLOGICAL & PHARMACEUTICAL BULLETIN | 2001年 / 24卷 / 07期

关键词：

ethaverine; papaverine; laudanosine; tetrahydropapaverine; kynuramine; monoamine oxidase;

D O I：

10.1248/bpb.24.838

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of benzylisoquinoline compounds such as ethaverine, laudanosine, and tetrahydropapaverine on monoamine oxidase (MAO, EC 1.4.3.4) activity in mouse brain were investigated, Ethaverine show ed an inhibition of MAO activity in a concentration-dependent manner (57.6% inhibition at 40 muM). Papaverine also inhibited MAO activity (38.1% inhibition at 40 muM). However, laudanosine and tetrahydropapaverine did not inhibit MAO activity. The IC50 value of ethaverine for MAO was 25.5 muM. Ethaverine non-competitively inhibited MAO activity with a substrate kynuramine. The K-i value for ethaverine was 11.9 muM. In addition, ethaverine proved to preferentially inhibit type B MAO activity in a concentration-dependent manner, with an IC50 value of 32.8 muM. These results suggest that ethaverine partially contributes to the regulation of catecholamine content.

引用

页码：838 / 840

页数：3

共 20 条

[1] INHIBITION OF MONOAMINE OXIDASE-A AND MONOAMINE OXIDASE-B BY SIMPLE ISOQUINOLINE ALKALOIDS - RACEMIC AND OPTICALLY-ACTIVE 1,2,3,4-TETRAHYDRO-ISOQUINOLINE, 3,4-DIHYDRO-ISOQUINOLINE, AND FULLY AROMATIC ISOQUINOLINE [J].