ArticleAnnals of translational medicine2021
Bepridil, a class IV antiarrhythmic agent, can block the TREK-1 potassium channel.
Article in Annals of translational medicine, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 authors at 2 institutions in 1 country.
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Abstract
backgroundThe 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.
methodsIn 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.
resultsIn 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
conclusionsBepridil may be a blocker for the TREK-1K
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