Inhibition of Ion Transport through Gramicidin A Channels by the Addition of Local Anesthetic Procaine,Electroanalysis

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Inhibition of Ion Transport through Gramicidin A Channels by the Addition of Local Anesthetic Procaine
Electroanalysis ( IF 2.7 ) Pub Date : 2017-12-13 , DOI: 10.1002/elan.201700609
Takuya Yamaguchi ₁ , Osamu Shirai ₁ , Yuki Kitazumi ₁ , Kenji Kano ₁

Affiliation

The blocking effects of the cationic procaine, a typical local anesthetic (LA), on ion transport through gramicidin A (gA) channels between two aqueous phases (W1 and W2) were electrochemically elucidated. Although the gA channels promoted the permeation of monovalent cations, especially Cs⁺, the addition of procaine to W1 decreased the permeation of Cs⁺ through these channels from W1 to W2. This can be explained based on the following mechanism. Hydrophobic cationic procaine tends to approach the pore of a gA channel. Since it is too large to enter the pore, it cannot pass through the channel. Thus, cationic procaine inhibits the permeation of Cs⁺ from W1 to W2 by competing with Cs⁺ for access to the entrances of the gA channels. It is postulated that the decrease in the apparent activity of Cs⁺ caused by this competition prevents ion transport through the gA channels.

中文翻译：

通过局部麻醉性普鲁卡因的抑制抑制通过杀螨素A通道的离子运输。

用电化学方法阐明了阳离子普鲁卡因（一种典型的局部麻醉药（LA））对通过短杆菌肽A（gA）通道在两个水相（W1和W2）之间进行离子迁移的阻断作用。尽管gA通道促进了单价阳离子（尤其是Cs ^+）的渗透，但向W1添加普鲁卡因降低了Cs ⁺通过这些通道从W1到W2的渗透。可以基于以下机制对此进行解释。疏水性阳离子普鲁卡因倾向于接近gA通道的孔。由于太大而无法进入孔，因此它无法通过通道。因此，阳离子普鲁卡因通过与Cs ⁺竞争来抑制Cs ⁺从W1到W2的渗透。用于访问gA通道的入口。据推测，由这种竞争引起的Cs ⁺表观活性的降低阻止了离子通过gA通道的迁移。

更新日期：2017-12-13

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