Schwarz S K, Puil E
Department of Pharmacology & Therapeutics, The University of British Columbia, Vancouver, Canada.
Br J Pharmacol. 1998 Aug;124(8):1633-42. doi: 10.1038/sj.bjp.0702015.
The effects of lignocaine [lidocaine] HCl (0.6 microM(-1) mM) on the membrane electrical properties and action potential firing of neurones of the ventral posterolateral (VPL) nucleus of the thalamus were investigated using whole cell recording techniques in rat brain slices in vitro. Bath application of lignocaine reversibly decreased the input resistance (Ri) of VPL neurones. This effect was observed at low, clinically sedative and analgesic concentrations (i.e., maximal amplitude at 10 microM) whereas higher concentrations (300 microM(-1) mM) had no effect on Ri. Lignocaine (10-100 microM) depolarized VPL neurones up to 14 mV in a reversible manner. Consistent with a decreased Ri, low concentrations of lignocaine shunted the current required for spike generation in the tonic pattern. Lignocaine increased the threshold amplitude of current required for firing and decreased the tonic firing frequency, without concomitant elevation of the voltage threshold for firing or reduction in the maximal rate of rise (dV/dt(max)) of spikes. Low concentrations of lignocaine shunted low threshold spike (LTS) burst firing evoked either from hyperpolarized potentials or as rebound bursts on depolarization from prepulse-conditioned potentials. Higher concentrations of lignocaine (300 microM - 1 mM), not associated with a decrease in Ri, elevated the voltage threshold for firing and reduced the dV/dt(max) of spikes in a concentration-dependent fashion. In conclusion, low concentrations of lignocaine shunted tonic and burst firing in VPL neurones by decreasing Ri, a mechanism not previously described for local anaesthetics in the CNS. We suggest that a decreased resistance in thalamocortical neurones contributes to the sedative, analgesic, and anaesthetic properties of systemic lignocaine in vivo.
采用体外大鼠脑片全细胞记录技术,研究了盐酸利多卡因(0.6微摩尔/升 - 1毫摩尔/升)对丘脑腹后外侧(VPL)核神经元膜电特性和动作电位发放的影响。浴槽给药利多卡因可使VPL神经元的输入电阻(Ri)可逆性降低。在低浓度(即临床镇静和镇痛浓度,10微摩尔时幅度最大)时可观察到这种效应,而较高浓度(300微摩尔/升 - 1毫摩尔/升)对Ri无影响。利多卡因(10 - 100微摩尔/升)可使VPL神经元可逆性去极化达14毫伏。与Ri降低一致,低浓度利多卡因使强直模式下产生动作电位所需的电流分流。利多卡因增加了发放所需电流的阈值幅度,降低了强直发放频率,而不伴有发放电压阈值的升高或动作电位最大上升速率(dV/dt(max))的降低。低浓度利多卡因可使由超极化电位诱发的低阈值尖峰(LTS)爆发性发放或由预脉冲条件电位去极化后的反弹爆发性发放分流。较高浓度的利多卡因(300微摩尔/升 - 1毫摩尔/升),与Ri降低无关,以浓度依赖方式提高了发放电压阈值并降低了动作电位的dV/dt(max)。总之,低浓度利多卡因通过降低Ri使VPL神经元的强直和爆发性发放分流,这是一种中枢神经系统中局部麻醉药以前未描述过的机制。我们认为丘脑皮质神经元电阻降低有助于体内系统性利多卡因的镇静、镇痛和麻醉特性。