乌拉坦对兴奋性和抑制性配体门控通道具有广泛的可检测的作用。作者运用全细胞膜片钳技术研究乌拉坦对wistar大鼠海马CA1神经元电压门控钠通道和动作电位的作用。结果发现乌拉坦可逆并剂量依赖性地抑制钠电流和动作电位,其中,在10mmol/L浓度时可减小钠电流强度达38%,使激活曲线向去极化方向移动,并延长钠通道失活后的恢复时间,降低动作电位的幅值。这些结果表明乌拉坦对电压门控钠通道的抑制作用可能是乌拉坦全身麻醉作用的机制之一。
Urethane has a wide spectrum of effects and affects both inhibitory and excitatory ligand-gated channels. The main aim of this study is to determine whether urethane can affect sodium channel which is a potential target for general anesthetic. The data show that urethane can reversibly inhibit sodium currents and single action potential in a concentration-dependent manner. With the concentrations used in the clinical study, urethane inhibited the peak amplitude of sodium current by 38%, shifted the activation curve towards the depolarizing potential, and prolonged the recovery of sodium channel from inactivation. It also depressed the amplitude of action potential. These results suggest that sodium channel may participate in the whole central nerves system depression by urethane.