Characterization of Stimulatory Action on Voltage-Gated Na⁺ Currents Caused by Omecamtiv Mecarbil, Known to Be a Myosin Activator.

ABSTRACT: Omecamtiv mecarbil (OM, CK-1827452) is recognized as an activator of myosin and has been demonstrated to be beneficial for the treatment of systolic heart failure. However, the mechanisms by which this compound interacts with ionic currents in electrically excitable cells remain largely unknown. The objective of this study was to investigate the effects of OM on ionic currents in GH3 pituitary cells and Neuro-2a neuroblastoma cells. In GH₃ cells, whole-cell current recordings showed that the addition of OM had different potencies in stimulating the transient (I_Na(T)) and late components (I_Na(L)) of the voltage-gated Na⁺ current (I_Na) with different potencies in GH₃ cells. The EC₅₀ value requir

SUBMITTER: Ting CY 

PROVIDER: S-EPMC10216194 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature