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[普鲁卡因和苯佐卡因对正常及乌头碱修饰的钠通道作用的比较研究]

[Comparative study of the action of procaine and benzocaine on normal and aconitine-modified sodium channels].

作者信息

Neguliaev Iu A, Nosyreva E D

出版信息

Tsitologiia. 1979 Jun;21(6):697-702.

PMID:462546
Abstract

Ionic currents of normal and aconitine modified sodium channels of the Ranvier node membrane were measured under voltage clamp conditions. The experiments with local anesthetics in the external Ringer solution have showed that dissociation constant (Kdis) of normal channel-anesthetic complex for procaine is 0.27 + 0.03 mM, and for benzocaine is 0.68 +/- 0.04 mM. With aconitine modified channels, Kdis increases and becomes 1.32 +/- 0.5 mM and 1.52 +/- 0.3 mM for procaine and benzocaine, respectively. It is ascertained that the development of aconitine effect is inhibited by neutral benzocaine to a lesser extent than by procaine. It is shown that the aconitine effect cannot be reversed by a high concentration of anesthetic. Hence, it appears that aconitine and anesthetic receptors do not coincide.

摘要

在电压钳制条件下测量了郎飞结膜正常和乌头碱修饰的钠通道的离子电流。在外部林格液中使用局部麻醉药的实验表明,正常通道 - 麻醉药复合物对普鲁卡因的解离常数(Kdis)为0.27±0.03 mM,对苯佐卡因的解离常数为0.68±0.04 mM。对于乌头碱修饰的通道,Kdis增加,普鲁卡因和苯佐卡因的Kdis分别变为1.32±0.5 mM和1.52±0.3 mM。已确定中性苯佐卡因对乌头碱作用发展的抑制程度小于普鲁卡因。结果表明,高浓度麻醉药不能逆转乌头碱的作用。因此,似乎乌头碱和麻醉药受体不一致。

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