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Wang Y, Fu Z, Ma Z, et al. Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel. Ann Transl Med. 2021;9(14):1123doi: 10.21037/atm-20-7971.
Wang, Y., Fu, Z., Ma, Z., Li, N., & Shang, H. (2021). Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel. Annals of translational medicine, 9(14), 1123. https://doi.org/10.21037/atm-20-7971
Wang, Ying, et al. "Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel." Annals of translational medicine vol. 9,14 (2021): 1123. doi: https://doi.org/10.21037/atm-20-7971
Wang Y, Fu Z, Ma Z, Li N, Shang H. Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel. Ann Transl Med. 2021 Jul;9(14):1123. doi: 10.21037/atm-20-7971. PMID: 34430564; PMCID: PMC8350656.
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Ann Transl Med. 2021 Jul;9(14):1123. doi: 10.21037/atm-20-7971.

Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel.

Annals of translational medicine

Ying Wang, Zhijie Fu, Zhiyong Ma, Na Li, Hong Shang

Affiliations

  1. Key Laboratory of Cardiovascular Remodeling and Function Research, Chinese Ministry of Education and Chinese Ministry of Public Health, Department of Cardiology, Qilu Hospital, Shandong University, Jinan, China.
  2. Department of Otorhinolaryngology, the First Affiliated Hospital of Shandong First Medical University, Jinan, China.
  3. Key Laboratory of Cardiovascular Proteomics of Shandong Province, Department of Geriatrics, Qilu Hospital, Shandong University, Jinan, China.

PMID: 34430564 PMCID: PMC8350656 DOI: 10.21037/atm-20-7971

Abstract

BACKGROUND: The TWIK-related potassium channel (TREK-1) can be regulated by different stimuli. However, it is not clear whether some antiarrhythmics affect the activity of TREK-1. In the present study, the effect of bepridil on the TREK-1 currents is investigated.

METHODS: In a TREK-1 stably-expressed HEK-293 cell line (HEK-TREK-1), U251MG cells, and isolated mouse ventricular myocytes, the TREK-1 current and action potentials were recorded by the patch-clamp technique. The standard voltage protocol was a 200 ms constant potential at 20 mV, followed bya 500 ms ramp from -90 to +20 mV (HEK-TREK-1) or +80 mV (U251MG cells and myocytes) every 10 s. The currents at +20 mV or +80 mV were used for analysis. The docking study of bepridil's binding model in the TREK-1 channel was performed using the Swissdock web service.

RESULTS: In HEK-TREK-1 cells, BL1249 induced a significantly large outwardly rectifying current with similar baseline TREK-1 current characteristic, with a reversal potential (-70 mV). The concentration of half-maximal activation (EC

CONCLUSIONS: Bepridil may be a blocker for the TREK-1K

2021 Annals of Translational Medicine. All rights reserved.

Keywords: TWIK-related potassium channel; antiarrhythmic drug; bepridil; patch clamp

Conflict of interest statement

Conflicts of Interest: All authors have completed the ICMJE uniform disclosure form (available at https://dx.doi.org/10.21037/atm-20-7971). The authors have no conflicts of interest to declare.

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