Heppner T J, Bonev A, Li J H, Kau S T, Nelson M T
Department of Pharmacology, University of Vermont, Colchester 05446, USA.
Pharmacology. 1996 Sep;53(3):170-9. doi: 10.1159/000139428.
The effects of Zeneca ZD6169, a tertiary carbinol, and levcromakalim were examined on the membrane potential of intact smooth muscle cells, and on ATP-sensitive K+ (KATP) channel currents in isolated smooth muscle cells from the guinea pig urinary bladder. ZD6169 and levcromakalim induced a glibenclamide-sensitive hyperpolarization of the membrane potential. The ZD6169- and levcromakalim-induced KATP currents were half-maximal at 1.02 and 2.63 mumol/l, respectively, with Hill coefficients of 1.46 and 1.62, respectively. The ZD6169-induced KATP currents were inhibited by internal ATP (3.0 mmol/l), reduced 34% by activators of protein kinase C, and decreased 35% when the external pH was lowered to 6.4. This study provides the first characterization of ZD6169 on KATP currents and indicates that ZD6169 is a potent opener of KATP channels in the smooth muscle from the urinary bladder.
研究了叔丁醇泽尼卡ZD6169和左卡尼汀对完整平滑肌细胞膜电位以及豚鼠膀胱分离平滑肌细胞中ATP敏感性钾通道（KATP）电流的影响。ZD6169和左卡尼汀诱导了格列本脲敏感的膜电位超极化。ZD6169和左卡尼汀诱导的KATP电流的半数最大效应浓度分别为1.02和2.63μmol/L，希尔系数分别为1.46和1.62。ZD6169诱导的KATP电流被胞内ATP（3.0 mmol/L）抑制，蛋白激酶C激活剂使其降低34%，当细胞外pH降至6.4时降低35%。本研究首次对ZD6169对KATP电流的作用进行了表征，并表明ZD6169是膀胱平滑肌中KATP通道的强效开放剂。
