The effect of HMS-01 on stably expressed hERG channel currents in HEK293 cells detected with the manualpatch clamp method

VernacularTitle:手动膜片钳检测HMS-01对HEK293细胞hERG通道电流的影响
Author: Huimin ZHANG ¹ ; Kefa XIANG ¹ ; Xiaofei SHI ¹ ; Zhen QIN ¹ ; Xia LIU ¹
Author Information

1. Department of Clinical Pharmacy, School of Pharmacy, Naval Medical University, Shanghai 200433, China.
Keywords: manualpatch clamp method; HEK293 cells; hERG channel
From: Journal of Pharmaceutical Practice 2022;40(2):132-135
CountryChina
Language:Chinese
Abstract: Objective To test the cardiac toxicity of new compound HMS-01 and evaluate the safety profile for clinical trials. Methods Manualpatch clamp method was used to measure human Ether-a-go-go-Related Gene (hERG) potassium channel currents with different concentrations of HMS-01. Cisapride was selected as the positive control drug. HMS-01 was diluted to the concentration of 0.3, 1, 3, 10 and 30 µmol/L and applied to the cells. The changes in electrical currents were recorded and the inhibition rate was calculated. Results At the highest concentration of 30µmol/L, the inhibitory rate of HMS-01 on hERG channel was less than 30%. There was no obvious inhibitory effect compared with cisapride. Conclusion Compared with the cisapride, HMS-01 has no obvious inhibitory effect on hERG channel and has no cardiotoxicity.