Connor E A, Levy S M, Parsons R L
J Physiol. 1983 Apr;337:137-58. doi: 10.1113/jphysiol.1983.sp014616.
The concentration- and voltage-dependent effects of atropine on the fast excitatory post-synaptic current (e.p.s.c.) of bullfrog sympathetic ganglion cells have been analysed and fitted to a kinetic scheme of open-channel blockade. Atropine (1-75 microM) reduced the peak e.p.s.c. amplitude without altering the quantal content or the reversal potential. The e.p.s.c. decay was complex in the presence of atropine, being well fitted by two exponential components. With increasing concentrations of atropine the time constant of the fast component, tau 2, decreased and the time constant of the slow component, tau 1, increased. Over the voltage range -30 to -100 mV tau 2 exhibited little or no voltage dependence and tau 1 increased with hyperpolarization. The amount of charge moved during the e.p.s.c. was reduced as a function of atropine concentration. Driving functions, which represented the rate of channel opening, were derived from e.p.s.c.s both from control and atropine-treated cells. The characteristics of the driving functions did not vary with membrane voltage, but the driving functions were shorter in duration from atropine-treated than control cells. The area under the driving function decreased as a function of atropine concentration. The decay time constants and the amplitude ratio of the exponential components were used to calculate the closing, blocking, and unblocking rate constants, alpha, G, and F. alpha and F remained constant with increasing atropine concentration, but G declined significantly. The voltage dependence of the equilibrium constant, G/F, implied that the transient blocking site for atropine is halfway through the ionic channel. The sequential model does not predict the concentration-dependent decrease in the blocking rate, G, or in the charge moved during an e.p.s.c. We conclude that atropine has an action more complex than simple channel blockade in sympathetic ganglion cells.
已分析了阿托品对牛蛙交感神经节细胞快速兴奋性突触后电流(e.p.s.c.)的浓度和电压依赖性效应,并将其拟合到开放通道阻断的动力学模型中。阿托品(1 - 75微摩尔)降低了e.p.s.c.的峰值幅度,而不改变量子含量或反转电位。在阿托品存在下,e.p.s.c.的衰减很复杂,由两个指数成分很好地拟合。随着阿托品浓度的增加,快速成分的时间常数τ2减小,而慢速成分的时间常数τ1增加。在 - 30至 - 100毫伏的电压范围内,τ2几乎没有或没有电压依赖性,而τ1随着超极化而增加。e.p.s.c.期间移动的电荷量随着阿托品浓度的增加而减少。代表通道开放速率的驱动函数来自对照细胞和阿托品处理细胞的e.p.s.c.。驱动函数的特征不随膜电压变化,但阿托品处理细胞的驱动函数持续时间比对照细胞短。驱动函数下的面积随着阿托品浓度的增加而减小。衰减时间常数和指数成分的幅度比用于计算关闭、阻断和解除阻断速率常数α、G和F。随着阿托品浓度的增加,α和F保持不变,但G显著下降。平衡常数G/F的电压依赖性表明,阿托品的瞬时阻断位点位于离子通道的中间。顺序模型无法预测阻断速率G或e.p.s.c.期间移动电荷的浓度依赖性降低。我们得出结论,阿托品在交感神经节细胞中的作用比简单的通道阻断更为复杂。