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Inhibitory effects of a TRPM4 inhibitor 9-phenanthrol on electrical activity of INS-1 pancreatic β-cells
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Hui-fang LIU, Cong-xiao ZHANG*, Ke-wei WANG*
Acta Pharmaceutica Sinica | 2023, 58(10) : 3059 - 3064
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Acta Pharmaceutica Sinica | 2023, 58(10): 3059-3064
Inhibitory effects of a TRPM4 inhibitor 9-phenanthrol on electrical activity of INS-1 pancreatic β-cells
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Hui-fang LIU, Cong-xiao ZHANG*, Ke-wei WANG*
Affiliations
  • School of Pharmacy, Qingdao University, Qingdao 266071, China
Published: 2023-10-12 doi: 10.16438/j.0513-4870.2023-0477
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The Ca2+-activated monovalent cation selective transient receptor potential melastatin 4 (TRPM4) channel expressed in pancreatic β-cells is implicated in the β-cell function and insulin secretion, but how pharmacological function of TRPM4 channel affects membrane excitability of β-cells remains largely unknown. Here, we report that pharmacological inhibition of TRPM4 by specific inhibitor 9-phenanthrol attenuates electrical activities of pancreatic β-cells. In whole-cell current clamp recordings, 9-phenanthrol results in inhibition of action potential frequency induced by tolbutamide of the INS-1 pancreatic β-cells in a dose-dependent manner with an IC50 value of 14.99 ± 7.93 μmol·L-1. Similarly, 9-phenanthrol also inhibited action potential firing in INS-1 cells stimulated by current injection. Further recordings of β-cells demonstrate the significant inhibitory effects on action potential peak and action potential amplitude by 9-phenanthrol. Taken together, our results show the involvement of TRPM4 channel function in pancreatic β-cells depolarization and action potential, it provides pharmacological experimental methods and theoretical support for the study of TRPM4 channel in pancreatic β-cells.

9-phenanthrol  /  transient receptor potential melastatin 4 channel  /  whole-cell current clamp  /  pancreatic β-cell  /  action potential
Hui-fang LIU, Cong-xiao ZHANG, Ke-wei WANG. Inhibitory effects of a TRPM4 inhibitor 9-phenanthrol on electrical activity of INS-1 pancreatic β-cells[J]. Acta Pharmaceutica Sinica, 2023 , 58 (10) : 3059 -3064 . DOI: 10.16438/j.0513-4870.2023-0477
Year 2023 volume 58 Issue 10
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doi: 10.16438/j.0513-4870.2023-0477
  • Receive Date:2023-04-19
  • Online Date:2025-11-21
  • Published:2023-10-12
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  • Received:2023-04-19
  • Revised:2023-06-19
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    School of Pharmacy, Qingdao University, Qingdao 266071, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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