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迈向早期安全性的新金标准：PatchLiner上的自动温控hERG测试。

Toward a New Gold Standard for Early Safety: Automated Temperature-Controlled hERG Test on the PatchLiner.

作者信息

Polonchuk Liudmila

机构信息

Non-Clinical Safety, Pharma Research, F. Hoffmann-La Roche Ltd. Basel, Switzerland.

出版信息

Front Pharmacol. 2012 Jan 26;3:3. doi: 10.3389/fphar.2012.00003. eCollection 2012.

DOI:10.3389/fphar.2012.00003
PMID:22303293
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3266667/
Abstract

The Patchliner® temperature-controlled automated patch clamp system was evaluated for testing drug effects on potassium currents through human ether-à-go-go related gene (hERG) channels expressed in Chinese hamster ovary cells at 35-37°C. IC(50) values for a set of reference drugs were compared with those obtained using the conventional voltage clamp technique. The results showed good correlation between the data obtained using automated and conventional electrophysiology. Based on these results, the Patchliner(®) represents an innovative automated electrophysiology platform for conducting the hERG assay that substantially increases throughput and has the advantage of operating at physiological temperature. It allows fast, accurate, and direct assessment of channel function to identify potential proarrhythmic side effects and sets a new standard in ion channel research for drug safety testing.

摘要

对Patchliner®温控自动膜片钳系统进行了评估，以测试药物对在35-37°C下中国仓鼠卵巢细胞中表达的人去甲肾上腺素能相关基因（hERG）通道钾电流的影响。将一组参考药物的半数抑制浓度（IC50）值与使用传统电压钳技术获得的值进行比较。结果表明，自动电生理技术与传统电生理技术所获数据之间具有良好的相关性。基于这些结果，Patchliner®代表了一种创新的自动电生理平台，用于进行hERG检测，该平台可大幅提高通量，并具有在生理温度下运行的优势。它能够快速、准确且直接地评估通道功能，以识别潜在的促心律失常副作用，并为药物安全性测试的离子通道研究设定了新的标准。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/80baa5ac347a/fphar-03-00003-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/771876c1f77c/fphar-03-00003-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/eb964abe8347/fphar-03-00003-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/2f1b2b07bdf5/fphar-03-00003-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/7439c6ee801b/fphar-03-00003-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/80baa5ac347a/fphar-03-00003-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/771876c1f77c/fphar-03-00003-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/eb964abe8347/fphar-03-00003-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/2f1b2b07bdf5/fphar-03-00003-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/7439c6ee801b/fphar-03-00003-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9bc1/3266667/80baa5ac347a/fphar-03-00003-g005.jpg

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