Verapamil inhibits Kir2.3 channels by binding to the pore and interfering with PIP₂ binding.

ABSTRACT: The inwardly rectifying potassium current of the cardiomyocyte (I_K1) is the main determinant of the resting potential. Ion channels Kir2.1, Kir2.2, and Kir2.3 form tetramers and are the molecular correlate of macroscopic I_K1 current. Verapamil is an antiarrhythmic drug used to suppress atrial and ventricular arrhythmias. Its primary mechanism of action is via blocking calcium channels. In addition, it has been demonstrated to block I_K1 current and the Kir2.1 subunit. Its effect on other subunits that contribute to I_K1 current has not been studied to date. We therefore analyzed the effect of verapamil on the Kir channels 2.1, 2.2, and 2.3 in the Xenopus oocyte expression system. Kir2.1, Kir2.2, and Kir2.3 channels were heterologously expressed in

SUBMITTER: Xynogalos P 

PROVIDER: S-EPMC10042922 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature