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aDepartment of Orthopaedic Surgery, Institute of Biomechanical Science and Biomechanical Key Laboratory of Hebei Province, Third Hospital of Hebei Medical University, Shijiazhuang, China
bThe Key Laboratory of Neural and Vascular Biology, Ministry of Education, Shijiazhuang, China
cDepartment of Biochemistry and Molecular Biology, Hebei Medical University, Shijiazhuang, China
dThe Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang, China
eDepartment of Pharmocology, Hebei Medical University, Shijiazhuang, China
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Article / Publication DetailsFirst-Page Preview
Received: March 25, 2022
Accepted: October 05, 2022
Published online: December 14, 2022
Number of Print Pages: 9
Number of Figures: 5
Number of Tables: 0
ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)
For additional information: https://www.karger.com/PHA
AbstractIntroduction: Voltage-gated Kv7/M potassium channels play an essential role in the control of membrane potential and neuronal excitability. Fangchinoline, a bisbenzylisoquinoline alkaloid, displays extensive biological activities including antitumor, anti-inflammatory, and antihypertension effects. In this study, we investigated the effects of fangchinoline on Kv7/M channels. Methods: A perforated whole-cell patch technique was used to record Kv7 currents from HEK293 cells and M-type currents from mouse dorsal root ganglion (DRG) neurons. Results: Fangchinoline inhibited Kv7.2/Kv7.3 currents in a concentration-dependent manner, with an IC50 of 9.5 ± 1.2 μM. Fangchinoline significantly inhibited Kv7.1, Kv7.2, Kv7.3, Kv7.4, and Kv7.3/Kv7.5 channels without selective effects. Furthermore, fangchinoline significantly slowed the activation of Kv7.1-Kv7.5 channels and inhibited native M-channel currents of DRG neurons. Conclusion: Taken together, our findings indicate that fangchinoline concentration-dependently inhibited Kv7/M channel currents.
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Received: March 25, 2022
Accepted: October 05, 2022
Published online: December 14, 2022
Number of Print Pages: 9
Number of Figures: 5
Number of Tables: 0
ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)
For additional information: https://www.karger.com/PHA
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