Morimura Kozo, Yamamura Hisao, Ohya Susumu, Imaizumi Yuji
Department of Molecular and Cellular Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya 467-8603, Japan.
J Pharmacol Sci. 2006 Mar;100(3):237-41. doi: 10.1254/jphs.sc0060011. Epub 2006 Mar 4.
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.
我们研究了小电导和中电导钙激活钾(SK和IK)通道开放剂DCEBIO(5,6 - 二氯 - 1 - 乙基 - 1,3 - 二氢 - 2H - 苯并咪唑 - 2 - 酮)和NS309(3 - 肟 - 6,7 - 二氯 - 1H - 吲哚 - 2,3 - 二酮)对L型钙通道电流(I(Ca))的影响,该电流是在全细胞电压钳制下从小鼠膀胱分离的平滑肌细胞中测量的。I(Ca)受到DCEBIO和NS309浓度依赖性抑制;半抑制浓度分别为71.6 μM和10.6 μM。NS309对IK通道相对于钙通道的特异性似乎较高,且高于DCEBIO。然而,当用作SK通道开放剂时,DCEBIO甚至NS309可能会显著阻断钙通道。