High throughput measurement of hERG drug block kinetics using the CiPA dynamic protocol [0.03%]
采用CiPA动态协议进行高通量hERG药物阻滞动力学测定
Monique J Windley,Jessica Farr,Clifford TeBay et al.
Monique J Windley et al.
The Comprehensive in vitro Proarrhythmic Assay (CiPA) has promoted use of in silico models of drug effects on cardiac repolarization to improve proarrhythmic risk prediction. These models contain a pharmacodynamic component describing drug ...
Drug-target interaction prediction using reliable negative samples and effective feature selection methods [0.03%]
一种基于可靠负样本和有效特征选择方法的药物-靶点相互作用预测方法
Mohammad Morovvati Sharifabad,Razieh Sheikhpour,Sajjad Gharaghani
Mohammad Morovvati Sharifabad
Machine learning-based approaches in the field of drug discovery have dramatically reduced the time and cost of the laboratory process of detecting potential drug-target interactions (DTIs). Standard binary classifiers require both positive...
Establishment of a new nonalcoholic steatohepatitis model; Ovariectomy exacerbates nonalcoholic steatohepatitis-like pathology in diabetic rats [0.03%]
建立一个新的非酒精性脂肪肝模型；卵巢切除加重糖尿病大鼠的非酒精性脂肪肝病理损害
Yasuka Saigo,Tomohiko Sasase,Kinuko Uno et al.
Yasuka Saigo et al.
An increasing number of patients worldwide are being diagnosed with nonalcoholic fatty liver disease and nonalcoholic steatohepatitis (NAFLD/NASH) because of the growing prevalence of obesity and metabolic disorders. The incidence of NAFLD ...
A method for assessing and monitoring consistency of nonclinical ECG analysis [0.03%]
一种评估和监测非临床心电图分析一致性的方法
Rebecca A Ross,C Michael Foley,Hilton M Jones et al.
Rebecca A Ross et al.
Cardiovascular safety is a key area of concern for new drugs in development, and the collection and analysis of electrocardiograms (ECGs) is a standard and major component of nonclinical testing. Digital data capture technology allows for h...
Development and validation of a LC-MS/MS method for simultaneous quantification of Ivabradine and Metoprolol in rat plasma [0.03%]
大鼠血浆中艾司洛尔和伊伐布雷定的LC-MS/MS同时定量测定方法的建立及验证
M Mukkanti Eswarudu,A Lakshmana Rao,K Vijay
M Mukkanti Eswarudu
The combination of Ivabradine (IVA) and Metoprolol (MET) was approved by US-FDA for symptomatic treatment of chronic stable angina pectoris. Hence, a potential analytical method that can simultaneously quantify these two drugs is required. ...
Preclinical nerve conduction: Nerve battery options for primate studies [0.03%]
灵长类动物神经传导的体外试验方法：感觉神经电池选择
Monica Metea,Ernesto Palmero-Soler,Lucas Crum
Monica Metea
Electrophysiological neurodiagnostic tests of nerve conduction (NC) are key assays included in preclinical safety and toxicology programs to assess the peripheral neuropathy (PN) liability of a new drug. Despite their increased use, standar...
Development of binary classification models for assessment of drug-induced liver injury in humans using a large set of FDA-approved drugs [0.03%]
基于大量FDA批准药物建立二分类模型评估人用药的肝损伤风险
Hui Zhang,Hong-Rui Zhang,Mei-Ling Hu et al.
Hui Zhang et al.
Drug-induced liver injury (DILI) has been identified as one of the major causes for drugs withdrawn from the market, and even termination during the late stages of development. Therefore, it is imperative to evaluate the DILI potential of l...
On the perspective of an aging population and its potential impact on drug attrition and pre-clinical cardiovascular safety assessment [0.03%]
老龄化人口视角及其对药物研发成功率和临床前心血管安全性评估的潜在影响
Bernard Fermini,Damian C Bell
Bernard Fermini
There is no refuting that America's population is growing older: for the first time in US history, by 2034 older adults (defined as >65 years of age) are projected to outnumber children under the age of 18, representing approximately 70 mil...
Diisopropylfluorophosphate (DFP) volatizes and cross-contaminates wells in a common 96-well plate format used in zebrafish larvae toxicology studies [0.03%]
二异丙基氟磷酸(DFP)在斑马鱼毒理学研究中常用的标准96孔板格式中挥发并交叉污染
Paige C Mundy,Rosalia Mendieta,Pamela J Lein
Paige C Mundy
Diisopropylfluorophosphate (DFP) is an organophosphate (OP) that is commonly used as a surrogate of OP nerve agents to study the neurotoxic effects of acute OP intoxication. In preliminary studies, we discovered abnormally high incidence of...
Accurate in silico simulation of the rabbit Purkinje fiber electrophysiological assay to facilitate early pharmaceutical cardiosafety assessment: Dream or reality? [0.03%]
兔浦肯野纤维电生理试验的精确计算机模拟在药物早期心脏安全性评估中的应用：梦想还是现实？
Marcel Mohr,Jean-Marie Chambard,Véronique Ballet et al.
Marcel Mohr et al.
As a branch of quantitative systems toxicology, in silico simulations are of growing attractiveness to guide preclinical cardiosafety risk assessments. Traditionally, a cascade of in vitro/in vivo assays has been applied in pharmaceutical r...