Azobenzene-Based Voltage-Gated Sodium Channel Blockers with Light-Controlled Local Anesthetic and Antiarrhythmic Activity

期刊论文
发表日期：

2024年6月1日

查看全文

A. N. Noev,
S. G. Kovalenko,
E. D. Gataulina,
E. A. Turchaninova,
V. D. Dzhabrailov,
A. A. Aitova,
D. A. Likhobabina,
J. A. Sutemieva,
S. R. Frolova,
L. E. Ruppel,
D. A. Minakov,
N. V. Suvorov,
P. V. Ostroverkhov,
Yu. L. Vasil’ev,
M. V. Nikolaev,
V. A. Tsvelaya,
K. I. Agladze,
M. A. Grin

摘要

Abstract

The work is devoted to the synthesis of new light-controlled voltage-gated sodium (Na_v) channel blockers based on azobenzene and the study of their local anesthetic and antiarrhythmic properties. The effect of ethercaine and two of its new derivatives on native Na_v channels was studied in vitro using the patch-clamp method on isolated excitable cells (neurons and cardiomyocytes) of a rat, and local anesthetic activity of the compounds was evaluated on rabbit’s eye cornea. Studies of the effect of the obtained compounds on the conductivity of excitation waves in cardiomyocyte cultures using the optical mapping method were performed. The effective light-dependent biological activity of ethercaine and its derivatives allows us to consider the resulting compounds as potential tools for light-controlled local anesthesia, as well as for non-invasive ablation of arrhythmia in the heart in cardiology.