新型钾通道开放剂AL0671对大鼠主动脉平滑肌细胞钾电流的影响。

The effect of AL0671, a novel potassium channel opener, on potassium current in rat aortic smooth muscle cells.

Matzno S, Sato R, Takai H, Aida Y, Karasaki S, Oyaizu M, Nakamura N, Katori R

Basic Research Laboratories, Green Cross Corporation, Osaka, Japan.

Gen Pharmacol. 1995 Oct;26(6):1327-34. doi: 10.1016/0306-3623(94)00282-r.

Abstract

We evaluated the mechanism of activation by AL0671, a novel potassium channel opener, of potassium current in rat aortic smooth muscle cells. 2. Under conditions of whole cell recording, AL0671 (1-1000 microM) markedly increased potassium current with a Hill coefficient of 2 and dissociation constant of 1.5 x 10(-4) M. This activation was completely inhibited by intracellular ATP. 3. Under inside-out patch conditions, the ATP-sensitive K+ channels (KATP) treated with AL0671 (100 microM) showed prolongation of the slower open time component and shortening of the slower closed time component without modification of channel conductance.

摘要

我们评估了新型钾通道开放剂AL0671对大鼠主动脉平滑肌细胞钾电流的激活机制。2. 在全细胞记录条件下，AL0671（1 - 1000微摩尔）显著增加钾电流，希尔系数为2，解离常数为1.5×10⁻⁴ M。这种激活被细胞内ATP完全抑制。3. 在膜内面向外的膜片钳条件下，用AL0671（100微摩尔）处理的ATP敏感性钾通道（KATP）显示较慢开放时间成分延长，较慢关闭时间成分缩短，而通道电导未改变。