首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >A comparison of the time course of excitation and inhibition by iontophoretic decamethonium in frog endplate.
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A comparison of the time course of excitation and inhibition by iontophoretic decamethonium in frog endplate.

机译:青蛙端板中离子电导十甲铵激发和抑制的时间过程的比较。

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摘要

1 The depolarization of frog endplate by a brief iontophoretic application of decamethonium was slower in time course than the inhibition of a long carbachol response produced by the same decamethonium pulse, or than the excitation produced by a brief equipotent carbachol pulse. 2 The delay between the peak inhibition and peak excitation produced by decamethonium, about 50 ms, is too great to be explained by slow receptor activation kinetics, since Katz & Miledi (1973) have shown that the lifetime of decamethonium-activated receptors is only 0.25 milliseconds. 3 If doses of carbachol and decamethonium are adjusted to give response amplitudes in the ratio corresponding to the ratio of their presumed maximum responses, then there is little difference in the time courses of the responses. 4 This observation, together with the finding that increasing the dose applied slows the decamethonium response much more than the carbachol response, suggests that a decamethonium response contains contributions from a much wider area of receptive membrane than does a carbachol response of equal amplitude. 5 Simulation shows that these geometrical effects are sufficient to account for the rapidity of inhibition compared to excitation without postulating slow receptor kinetics. 6 It is pointed out that similar effects may account for certain results obtained in iontophoretic studies of desensitization.
机译:1通过短暂地离子电渗入十甲基甲铵对青蛙终板进行去极化,其时间过程比抑制相同十甲基甲铵脉冲产生的长卡巴胆碱响应或抑制短暂的等电位卡巴胆碱脉冲产生的激发慢。 2十甲基铵产生的峰抑制与峰激发之间的延迟(大约50毫秒)太大,无法用缓慢的受体激活动力学来解释,因为Katz&Miledi(1973)表明十甲基激活的受体的寿命只有0.25毫秒。 3如果调整了卡巴胆碱和十甲铵的剂量,以使其响应幅度对应于假定的最大响应之比,则响应的时间过程几乎没有差异。 [4]该观察结果以及增加施用剂量使十甲铵盐的响应比咔唑醇的响应减慢得多的发现表明,十甲铵铵的响应膜比等幅度的甲酰胆碱的响应具有更大的感受膜面积。 5仿真表明,与激发相比,这些几何效应足以说明抑制的快速性,而不会假定受体动力学缓慢。 6指出类似的作用可能解释了脱敏在离子电渗疗法研究中获得的某些结果。

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