Selective activation of vascular K_v 7.4/K_v 7.5 K⁺ channels by fasudil contributes to its vasorelaxant effect.

ABSTRACT:

Background and purpose

K_v 7 (K_v 7.1-7.5) channels play an important role in the regulation of neuronal excitability and the cardiac action potential. Growing evidence suggests K_v 7.4/K_v 7.5 channels play a crucial role in regulating vascular smooth muscle contractility. Most of the reported K_v 7 openers have shown poor selectivity across these five subtypes. In this study, fasudil - a drug used for cerebral vasospasm - has been found to be a selective opener of K_v 7.4/K_v 7.5 channels.

Experimental approach

A perforated whole-cell patch technique was used to record the currents and membrane potential. Homology modelling and a docking technique were used to investigate the interaction between fasudil

SUBMITTER: Zhang X 

PROVIDER: S-EPMC5120158 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature