过刊浏览

激活#delta#阿片受体可抑制大鼠心室肌细胞L--型钙电流和瞬时外向钾电流

林媛媛, 武冬梅, 刘磊, 刘清华, 闫喆一, 吴博威

山西医科大学生理学教研室.山西,太原 030001；山西医科大学药理学教研室.山西,太原 030001

摘要

该研究采用全细胞膜片钳技术观察了SNC162（一种选择性#delta#阿片受体激动剂）对大鼠心室肌细胞L型钙电流（L--type Ca~(2+) current，I_(Ca-L)）和瞬时外向钾电流（transient outward K~(+) current，I_(to)）的影响。结果显示，SNC162明显抑制大鼠心室肌细胞I_(Ca-L)和I_(to)，对I_(Ca-L)和I_(to)的最大抑制率分别为（46.13±4.12）％和（36.53±10.57）％。1×10~(-4)mol／L SNC162使I_(Ca-L)的平均电流密度从（8.98±0.40）pA／pF下降到（4.84±0.44）pA／pF（{sl P}<0.01，{sl n}=5），I_(to)的平均电流密度从（18.69±2.42）pA／pF降低到（11.73±1.67）pA／pF（{sl P}<0.01，{sl n}=5）。单独应用naltrindole（一种选择性#delta#阿片受体拮抗剂）对大鼠心室肌细胞I_(Ca-L)和I_(to)无显著作用，但预先应用naltrindole可以消除SNC162对I_(Ca-L)和I_(to)的抑制作用。结果表明，通过#delta#阿片受体，SNC162（1×10~(-6)---1×10~(-4)mol／L）浓度依赖性地抑制大鼠心室肌细胞I_(Ca-L)和I_(to)，这可能是激动#delta#阿片受体产生抗心律失常效应的重要机制。

关键词： SNC162; 膜片钳技术; 心肌细胞; naltrindole

Activation of #delta#--opioid receptors inhibits L--type Ca~(2+) current and transient outward K~(+) current in rat ventricular myocytes

Lin Yuanyuan, Wu Dongmei, Liu Lei, Liu Qinghua, Yan Zheyi, Wu Bowei

Department of Physiology,Shanxi Medical University.Taiyuan 030001,Shanxi；China

Abstract

In the present study, whole-cell patch-clamp technique was used to observe the effects of SNC162, a selective agonist of #delta#-opioid receptors, on L-type Ca~(2+) current （I_(Ca-L)） and transient outward K~(+) current （I_(to)） in rat ventricular myocytes. The results showed that SNC162 significantly inhibited I_(Ca-L) and Ito in rat ventricular myocytes. The maximal inhibition rate of I_(Ca-L) and Ito reached （46.13±4.12）% and （36.53±10.57）%, respectively. SNC162 at 1×10~(-4) mol/L inhibited the current density of I_(Ca-L) from （8.98±0.40）pA/pF to （4.84±0.44）pA/pF （P〈0.01, n=5） and inhibited that of I_(to) from （18.69±2.42）pA/pF to （11.73±1.67）pA/pF （P〈0.01, n=5）. Furthermore, the effects of naltrindole, a highly selective antagonist of #delta#-opioid receptors, on I_(Ca-L) and I_(to) were also observed. The results showed that naltrindole alone had no effects on I_(Ca-L) and I_(to), while it abolished the inhibitory effects of SNC162 on I_(Ca-L) and I_(to). In conclusion, SNC162 concentration-dependently inhibited I_(Ca-L) and I_(to) in rat ventricular myocytes via activation of the #delta#-opioid receptors, which may be a fundamental mechanism underlying the antiarrhythmic effect of activating #delta#-opioid receptors.

Key words: SNC162;patch-clamp technique;myocytes;cardiac

收稿日期：　　录用日期：

通讯作者：　　E-mail:

引用本文：

林媛媛, 武冬梅, 刘磊, 刘清华, 闫喆一, 吴博威. 激活#delta#阿片受体可抑制大鼠心室肌细胞L--型钙电流和瞬时外向钾电流[J]. 生理学报 2008; 60 (1): 38-42.

Lin Yuanyuan, Wu Dongmei, Liu Lei, Liu Qinghua, Yan Zheyi, Wu Bowei. Activation of #delta#--opioid receptors inhibits L--type Ca~(2+) current and transient outward K~(+) current in rat ventricular myocytes. Acta Physiol Sin 2008; 60 (1): 38-42 (in Chinese with English abstract).