...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Clinical and experimental pharmacology & physiology >Pro- and anti-arrhythmic effects of a kappa opioid receptor agonist: a model for the biphasic action of a local hormone in the heart.
【24h】

Pro- and anti-arrhythmic effects of a kappa opioid receptor agonist: a model for the biphasic action of a local hormone in the heart.

机译：κ阿片受体激动剂的抗心律失常作用：心脏局部激素双相作用的模型。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

1. The effects of kappa opioid receptor stimulation on cardiac rhythm and the underlying signal pathways were investigated in the rat. 2. Stimulation of kappa opioid receptors with 40-50 mumol/L U50 488H, a selective kappa opioid receptor agonist, induced dysrhythmias and increased inositol 1,4,5-trisphosphate (IP3) production in rat isolated, perfused heart. The pro-arrhythmic effects of U50 488H were abolished by 5 mumol/L norbinaltorphimine (nor-BNI), a specific kappa opioid receptor antagonist. 3. The effect of U50 488H on cardiac dysrhythmia and IP3 production were abolished by 1 mmol/L neomycin and streptomycin, phospholipase C (PLC) inhibitors. 4. At 1 mumol/L, U50 488H, which itself has no effect on cardiac rhythm and IP3 production, significantly attenuated the potentiating effect of 1 mumol/L noradrenaline (NA) on dysrhythmias, which were induced by low flow in the isolated heart. The effects of U50 488H were abolished by 1 mumol/L nor-BNI. Cytosolic cAMP production was augmented by 1 mumol/L NA and this was significantly attenuated by 1 mumol/L U50 488H. 5. At 1 mumol/L, U50 488H also reduced [Ca2+]i oscillations induced by 0.5 mumol/L NA and 0.5 mumol/L forskolin, an activator of adenylate cyclase (AC). 6. In conclusion, U50 488H exerted pro- and anti-arrhythmic actions at high and lower concentrations, respectively. The former effect was mediated via the PLC/IP3 pathway, while the latter was mediated via the AC/cAMP pathway.
机译：1.在大鼠中研究了κ阿片受体刺激对心律和潜在信号通路的影响。 2.用40-50μmol/ L U50 488H（一种选择性阿片受体激动剂）刺激大鼠阿片受体，诱导离体性心律失常，并增加大鼠离体灌流心脏中的肌醇1,4,5-三磷酸（IP3）产生。 U50 488H的心律失常作用被5μmol/ L降冰片碱（nor-BNI）（一种特定的阿片类阿片受体拮抗剂）取消。 3. 1 mmol / L新霉素和链霉素，磷脂酶C（PLC）抑制剂消除了U50 488H对心律不齐和IP3产生的影响。 4.在1μmol/ L时，U50 488H本身对心律和IP3的产生没有影响，但显着减弱了1 mumol / L去甲肾上腺素（NA）对心律失常的增强作用，这是由于离体心脏的低流量引起的。 1 mumol / L nor-BNI消除了U50 488H的作用。细胞溶质中cAMP的产量增加了1μmol/ L NA，而被1μmol/ L U50 488H显着减弱了。 5.在1μmol/ L下，U50 488H还减少了0.5μmol/ L NA和0.5μmol/ L毛喉素（腺苷酸环化酶（AC）的激活剂）诱导的[Ca2 +] i振荡。 6.总之，U50 488H在高和低浓度下分别发挥了抗心律失常的作用。前者是通过PLC / IP3途径介导的，后者是通过AC / cAMP途径介导的。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号