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Peer-reviewedCC BY-NCEuropean journal of histochemistry : EJH

Short- and long-term effects of dronedarone on Cav3.1- and Cav3.2-T-type calcium channel current.

  • Xuan Jiang1
  • Jianan Xu2
  • Honghou He2
  • Zelong Cao2
  • Da Liu2
  • Zhiyan Chen2
  • Ligang Ding3
  • Mingqi Zheng2
  1. 1Postdoctoral Mobile Station, The First Hospital of Hebei Medical University, Shijiazhuang, Hebei.
  2. 2Department of Cardiology, The First Hospital of Hebei Medical University, Shijiazhuang, Hebei.
  3. 3Arrhythmia Center, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, Xicheng District, Beijing.
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Abstract

T-type calcium channels (TTCCs), including the Cav3.1 and Cav3.2 subtypes, play a critical role in regulating cardiac electrical activity. Their abnormal expression is closely associated with arrhythmias and cardiac dysfunction caused by myocardial infarction (MI). Dronedarone, a multi-target antiarrhythmic drug, is widely used to treat atrial fibrillation and atrial flutter but has shown adverse effects under pathological conditions such as MI. This study aims to investigate the direct effects and underlying mechanisms of dronedarone on TTCCs. Using neonatal rat cardiomyocytes, HEK293T cells transfected with Cav3.1 and Cav3.2, and MI rat model, we systematically analyzed the effects of dronedarone on TTCC activity. Dronedarone significantly inhibited Cav3.2 channel activity with an IC50 of 9.20 µM, while its effect on Cav3.1 was weaker (IC50 = 46.41 µM). Chronic treatment with dronedarone also slowed the activation and inactivation kinetics of TTCCs. In vivo experiments demonstrated that dronedarone exacerbated myocardial damage and fibrosis in the MI model. These findings suggest that dronedarone inhibits TTCC activity, particularly the Cav3.2 subtype, and alters its kinetic properties. This study reported the electrophysiological effects of dronedarone on T-type calcium channels, providing new insights into its electrophysiological properties and potential role in adverse cardiac events.

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Cite

BibTeXRIS
BibTeX
@article{jiang2026short,
  title = {{Short- and long-term effects of dronedarone on Cav3.1- and Cav3.2-T-type calcium channel current.}},
  author = {Xuan Jiang and Jianan Xu and Honghou He and Zelong Cao and Da Liu and Zhiyan Chen and Ligang Ding and Mingqi Zheng},
  journal = {European journal of histochemistry : EJH},
  year = {2026},
  month = oct,
  doi = {10.4081/ejh.2026.4534},
  url = {https://europepmc.org/article/MED/42898062},
  note = {CC BY-NC},
}
RIS
TY  - JOUR
TI  - Short- and long-term effects of dronedarone on Cav3.1- and Cav3.2-T-type calcium channel current.
AU  - Xuan Jiang
AU  - Jianan Xu
AU  - Honghou He
AU  - Zelong Cao
AU  - Da Liu
AU  - Zhiyan Chen
AU  - Ligang Ding
AU  - Mingqi Zheng
PY  - 2026
DA  - 2026/10/20
JO  - European journal of histochemistry : EJH
DO  - 10.4081/ejh.2026.4534
UR  - https://europepmc.org/article/MED/42898062
AB  - T-type calcium channels (TTCCs), including the Cav3.1 and Cav3.2 subtypes, play a critical role in regulating cardiac electrical activity. Their abnormal expression is closely associated with arrhythmias and cardiac dysfunction caused by myocardial infarction (MI). Dronedarone, a multi-target antiarrhythmic drug, is widely used to treat atrial fibrillation and atrial flutter but has shown adverse effects under pathological conditions such as MI. This study aims to investigate the direct effects and underlying mechanisms of dronedarone on TTCCs. Using neonatal rat cardiomyocytes, HEK293T cells transfected with Cav3.1 and Cav3.2, and MI rat model, we systematically analyzed the effects of dronedarone on TTCC activity. Dronedarone significantly inhibited Cav3.2 channel activity with an IC50 of 9.20 µM, while its effect on Cav3.1 was weaker (IC50 = 46.41 µM). Chronic treatment with dronedarone also slowed the activation and inactivation kinetics of TTCCs. In vivo experiments demonstrated that dronedarone exacerbated myocardial damage and fibrosis in the MI model. These findings suggest that dronedarone inhibits TTCC activity, particularly the Cav3.2 subtype, and alters its kinetic properties. This study reported the electrophysiological effects of dronedarone on T-type calcium channels, providing new insights into its electrophysiological properties and potential role in adverse cardiac events.
SN  - 1121-760X
SN  - 2038-8306
ER  -