Inhibition of K-ATP channel activity by troglitazone in CRI-G1 insulin-secreting cells

被引：26

作者：

Lee, K ^{[1
]}

Ibbotson, T ^{[1
]}

Richardson, PJ ^{[1
]}

Boden, PR ^{[1
]}

机构：

[1] UNIV CAMBRIDGE,DEPT PHARMACOL,CAMBRIDGE CB2 1QJ,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1996年 / 313卷 / 1-2期

关键词：

troglitazone; K-ATP channel; beta cell; insulin secretion;

D O I：

10.1016/0014-2999(96)00619-X

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Patch-clamp recording techniques were used to examine the effect of troglitazone on K-ATP channel activity in Cambridge rat insulinoma-G1 (CRI-G1) insulin-secreting cells. In both inside-out and outside-out patch recordings, bath application of troglitazone reduced K-ATP channel activity. This inhibition was independent of the membrane voltage and was poorly reversible. In whole-cell studies, troglitazone inhibited K-ATP channel currents with an IC50 of 697 +/- 92nM and an associated Hill coefficient of 1.2 +/- 0.2. In current clamp recordings 10 mu M troglitazone depolarised the CRI-G1 cell membrane by 36.8 +/- 3.9 mV with a concomitant decrease in membrane conductance. However, in contrast to the rapid depolarisation produced by tolbutamide, the effects of troglitazone developed more slowly, usually taking 15-20 min to develop.

引用

页码：163 / 167

页数：5

共 14 条

[1] 5 NEW INSULIN-PRODUCING CELL-LINES WITH DIFFERING SECRETORY PROPERTIES [J].