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首页> 外文期刊>Acta Pharmacologica Sinica >Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017
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Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017

机译：CPU 86017阻断心肌L型钙通道和钙诱导的血管平滑肌收缩

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AIM: To assess the blockade by CPU 86017 on the L-type calcium channels in the myocardium and on the Ca~(2+)-related contractions of vascular smooth muscle. METHODS: The whole-cell patch-clamp was applied to investigate the blocking effect of CPU 86017 on the L-type calcium current in isolated guinea pig myocytes and contractions by KC1 or phenylephrine (Phe) of the isolated rat tail arteries were measured. RESULTS: Suppression of the L-type current of the isolated myocytes by CPU 86017 was moderate, in time- and concentration-dependent manner and with no influence on the activation and inactivation curves. The IC_(50) was 11.5 μmol/L. Suppressive effect of CPU 86017 on vaso-contractions induced by KC1 100 mmol/L, phenylephrine 1 μmol/L in KH solution (phase 1), Ca~(2+) free KH solution ( phase 2), and by addition of CaCl_2 into Ca~(2+)-free KH solution (phase 3) were observed. The IC_(50) to suppress vaso-contractions by calcium entry via the receptor operated channel (ROC) and voltage-dependent channel (VDC) was 0.324 μmol/L and 16.3 μmol/L, respectively. The relative potency of CPU 86017 to suppress vascular tone by Ca~(2+) entry through ROC and VDC is 1/187 of prazosin and 1/37 of verapamil, respectively. CONCLUSION: The blocking effects of CPU 86017 on the L-type calcium channel of myocardium and vessel are moderate and non-selective. CPU 86017 is approximately 50 times more potent in inhibiting ROC than VDC.
机译：目的：评估CPU 86017对心肌L型钙通道和血管平滑肌Ca〜（2+）相关收缩的阻滞作用。方法：采用全细胞膜片钳研究CPU 86017对豚鼠心肌细胞L型钙电流的阻断作用，并测定KC1或去氧肾上腺素（Phe）对大鼠尾动脉的收缩作用。结果：CPU 86017对分离的心肌细胞的L型电流的抑制作用是中等的，呈时间和浓度依赖性，对激活和失活曲线没有影响。 IC_（50）为11.5μmol/ L。 CPU 86017对KH1 100 mmol / L，去氧肾上腺素1μmol/ L的KH溶液（第1阶段），不含Ca〜（2+）的KH溶液（第2阶段）以及向其中添加CaCl_2引起的血管收缩的抑制作用观察到无Ca〜（2+）的KH溶液（第3阶段）。抑制钙通过受体操作通道（ROC）和电压依赖性通道（VDC）进入血管收缩的IC_（50）分别为0.324μmol/ L和16.3μmol/ L。 CPU 86017通过Ca〜（2+）通过ROC和VDC抑制血管紧张的相对效力分别为哌唑嗪的1/187和维拉帕米的1/37。结论：CPU 86017对心肌和血管L型钙通道的阻滞作用是中等且非选择性的。 CPU 86017的ROC抑制能力是VDC的50倍。

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