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hERGAPDbase:一个记录 hERG 通道抑制潜力和化合物致 APD 延长活性的数据库。

hERGAPDbase: a database documenting hERG channel inhibitory potentials and APD-prolongation activities of chemical compounds.

机构信息

Department of Genetic Resources Technology, Faculty of Agriculture, Kyushu University, 6-10-1 Hakozaki, Higashi-ku, Fukuoka 812-8581, Japan.

出版信息

Database (Oxford). 2011 May 17;2011:bar017. doi: 10.1093/database/bar017. Print 2011.

Abstract

Drug-induced QT interval prolongation is one of the most common reasons for the withdrawal of drugs from the market. In the past decade, at least nine drugs, i.e. terfenadine, astemizole, grepafloxacin, terodiline, droperidol, lidoflazine, sertindole, levomethadyl and cisapride, have been removed from the market or their use has been severely restricted because of drug-induced QT interval prolongation. Therefore, this irregularity is a major safety concern in the case of drugs submitted for regulatory approval. The most common mechanism of drug-induced QT interval prolongation may be drug-related inhibition of the human ether-á-go-go-related gene (hERG) channel, which subsequently results in prolongation of the cardiac action potential duration (APD). hERGAPDbase is a database of electrophysiological experimental data documenting potential hERG channel inhibitory actions and the APD-prolongation activities of chemical compounds. All data entries are manually collected from scientific papers and curated by a person. With hERGAPDbase, we aim to provide useful information for chemical and pharmacological scientists and enable easy access to electrophysiological experimental data on chemical compounds. Database URL: http://www.grt.kyushu-u.ac.jp/hergapdbase/.

摘要

药物引起的 QT 间期延长是药物从市场撤出的最常见原因之一。在过去的十年中,至少有九种药物,即特非那定、阿司咪唑、格帕沙星、特罗地林、氟哌利多、利福喷汀、塞替啶、左美丙嗪和西沙必利,由于药物引起的 QT 间期延长已从市场上撤出或其使用受到严格限制。因此,这种不规则性是药物监管批准申请中的一个主要安全问题。药物引起的 QT 间期延长的最常见机制可能是药物相关的人类 ether-á-go-go 相关基因 (hERG) 通道抑制,随后导致心脏动作电位持续时间 (APD) 延长。hERGAPDbase 是一个电生理实验数据数据库,记录了潜在的 hERG 通道抑制作用和化合物的 APD 延长活性。所有数据条目都是从科学论文中手动收集并由专人整理的。使用 hERGAPDbase,我们旨在为化学和药理学科学家提供有用的信息,并使他们能够方便地访问有关化合物的电生理实验数据。数据库网址:http://www.grt.kyushu-u.ac.jp/hergapdbase/。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f590/3096323/d3e23e1eea5b/bar017f1.jpg

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