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首页> 外文期刊>Journal of pharmacological sciences. >Voltage-dependent Ca2+-channel block by openers of intermediate and small conductance Ca2+-activated K+ channels in urinary bladder smooth muscle cells.
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Voltage-dependent Ca2+-channel block by openers of intermediate and small conductance Ca2+-activated K+ channels in urinary bladder smooth muscle cells.

机译:电压依赖性Ca2 +通道被膀胱平滑肌细胞中和小电导Ca2 +激活的K +通道的开启剂阻断。

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摘要

We examined effects of small and intermediate conductance Ca(2+)-activated K(+) (SK and IK) channel openers, DCEBIO (5,6-dichloro-1-ethyl-1,3-dihydro-2H-benzimidazol-2-one) and NS309 (3-oxime-6,7-dichloro-1H-indole-2,3-dione), on L-type Ca(2+) channel current (I(Ca)) that was measured in smooth muscle cells isolated from mouse urinary bladder under whole cell voltage-clamp. The I(Ca) was concentration-dependently inhibited by DCEBIO and NS309; half inhibition was obtained at 71.6 and 10.6 muM, respectively. The specificity of NS309 to the IK channel over the Ca(2+) channel appears to be high and higher than that of DCEBIO. DCEBIO and even NS309 may, however, substantially block Ca(2+) channels when used as SK channel openers.
机译:我们检查了中小电导Ca(2+)激活的K(+)(SK和IK)通道开放剂DCEBIO(5,6-dichloro-1-ethyl-1,3-dihydro-2H-benzimidazol-2 -一个)和NS309(3-肟-6,7-dichloro-1H-吲哚-2,3-dione),在平滑肌上测量的L型Ca(2+)通道电流(I(Ca))在全细胞电压钳下从小鼠膀胱分离的细胞。 I(Ca)被DCEBIO和NS309浓度依赖性抑制。在71.6和10.6μM下分别获得一半抑制。 NS309对IK通道在Ca(2+)通道上的特异性似乎很高,也比DCEBIO高。但是,DCEBIO甚至NS309用作SK通道开放剂时,可能会基本上阻塞Ca(2+)通道。

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