A NOVEL ETA ANTAGONIST (BQ-123) INHIBITS ENDOTHELIN-1-INDUCED PHOSPHOINOSITIDE BREAKDOWN AND DNA-SYNTHESIS IN RAT VASCULAR SMOOTH-MUSCLE CELLS

被引：95

作者：

EGUCHI, S

HIRATA, Y

IHARA, M

YANO, M

MARUMO, F

机构：

[1] TOKYO MED & DENT UNIV,DEPT INTERNAL MED 2,DIV ENDOCRINE HYPERTENS,1-5-45 YUSHIMA,BUNKYO KU,TOKYO 113,JAPAN

[2] BANYO PHARMACEUT CO,CENT RES LABS,MEGURO KU,TOKYO 153,JAPAN

来源：

FEBS LETTERS | 1992年 / 302卷 / 03期

关键词：

ENDOTHELIN-1; RECEPTOR ANTAGONIST; INOSITOL TRISPHOSPHATE; DNA SYNTHESIS; VASCULAR SMOOTH MUSCLE CELL;

D O I：

10.1016/0014-5793(92)80451-L

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：

The effects of a novel cyclic pentapeptide (BQ-123), an endothelin (ET) antagonist selective for the ET(A) receptor subtype, on phosphoinositide breakdown and DNA synthesis stimulated by ET-1 were studied in cultured rat vascular smooth muscle cells (VSMC). BQ-123 competitively inhibited the binding of [I-125]ET-1 to VSMC with the apparent K(i) of 4 x 10(-9) M. BQ-123 dose-dependently inhibited formation of inositol-1,4,5-trisphosphate and [H-3]thymidine uptake stimulated by ET-1. These data suggest that the ET-1-induced DNA synthesis in VSMC is mainly mediated by ET(A) receptor subtype.

引用

收藏

页码：243 / 246

页数：4

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