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Electrophysiological characterization of the state-dependent inhibition of Kv7.1 and I<sub>Ks</sub> by UCL2077.


ABSTRACT: In cardiomyocytes, Kv7.1 associates with the regulatory subunit KCNE1 to generate the delayed rectifier potassium current IKs, which plays a crucial role in cardiac repolarization at elevated heart rates. Gain-of-function mutations in either of these subunits are associated with short QT syndrome, a condition that increases the risk of cardiac arrhythmias including atrial fibrillation, syncope, and sudden death. Therefore, the study of pharmacological inhibitors of Kv7.1 and IKs is of significant therapeutic interest. In this work, we used whole-cell patch clamp recordings to characterize the electrophysiological effects of the Kv7.1 blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077) in both Kv7.1 and IKs (Kv7.1 + KCNE1) channels. We found that UCL207

SUBMITTER: Sastre D 

PROVIDER: S-EPMC12799529 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature