FluxOR^(TM) Thallium Assay Kits在药物安全性筛选方面的应用  

Application of FluxOR^(TM) Thallium Assay Kits in Drug Safety Screening

作　　者：张雪荣[1] 郝六平[1] 张之东[1] 马丽锋[1] 

机构地区：[1]河北化工医药职业技术学院制药工程系,河北石家庄050026

出　　处：《河北师范大学学报（自然科学版）》2010年第5期583-586,共4页Journal of Hebei Normal University：Natural Science

摘　　要：以稳定表达人类的hERG基因的中国仓鼠卵巢细胞(CHO-K1)为材料,使用FluxORTMThallium Assay Kits检测西沙比利和多菲利特对hERG通道的抑制性.以此系统为基础,检测本实验室合成的5个新化合物对hERG通道的作用.实验结果显示,西沙比利和多菲利特对hERG通道的IC50分别为86.7,28.1 nmol/L;5种化合物HBHG2201,HBHG1013,HBHG2311,HBHG1023,HBHG2108对hERG通道的抑制率分别为-2.34%,78.0%,23.8%,44.2%和49.8%.FluxORTM Thallium Assay Kits系统可用于药物研发安全性筛选,以评估化合物潜在的hERG毒性.CHO-K1（Chinese Hamster Ovary cell） expressing hERG（human ether-a-go-go-related gene） was used as the host cell,in FluxORTM Thallium Assay Kits,to appraise the effect of hERG by Cisapride and Dofetilide.At the sametime,the inhibition of HBHG2201,HBHG1013,HBHG2311,HBHG1023 and HBHG2108 was tested.The IC50 values of Cisapride and Dofetilide 86.7,28.1 nmol/L,and the inhibition ratio of HBHG2201,HBHG1013,HBHG2311,HBHG1023 and HBHG2108（10 μmol/L） were-2.34 %,78.0 %,23.8 %,44.2 %和49.8 % respectively.FluxORTM Thallium Assay Kits could be used to Drug RD Safety Screening to evaluate the compounds＇ hERG toxicity.

关 键 词：安全性筛选 CHO-K1 HERG FluxORTM 

分 类 号：R965.1[医药卫生—药理学]