Results 21 to 30 of about 103,612 (260)
An Ultrafast UPLC–MS/MS Method for Characterizing the In Vitro Metabolic Stability of Acalabrutinib
Molecules, 2023 Acalabrutinib, commercially known as Calquence®, is a pharmacological molecule that has robust inhibitory activity against Bruton tyrosine kinase. The medicine in question was carefully developed by the esteemed pharmaceutical company AstraZeneca.
Mohamed W. Attwa +3 more
doaj +1 more source
The Specific Mechanism of TREM2 Regulation of Synaptic Clearance in Alzheimer’s Disease
Frontiers in Immunology, 2022 Alzheimer’s disease (AD) is a progressive neurodegenerative disease. Synaptic dysfunction is an integral feature of AD pathophysiology and a significant factor in early cognitive impairment in AD.
Qi Qin +5 more
doaj +1 more source
Using partition analysis as a facile method to derive net clearances
Clinical and Translational Science, 2022 Partition analysis has been described previously by W.W. Cleland to derive net rate constants and simplify the derivation of enzyme kinetic equations. Here, we show that partition analysis can be used to derive elimination and transfer (distribution) net
Ken Korzekwa, Jaydeep Yadav, Swati Nagar
doaj +1 more source
Simplifying the Execution of HepatoPac MetID Experiments: Metabolite Profile and Intrinsic Clearance Comparisons [PDF]
Drug Metabolism and Disposition, 2020 The HepatoPac micropatterned coculture (MPCC) hepatocyte system has been shown to be an effective tool to investigate the qualitative human and preclinical species' metabolite profiles of new drug candidates. However, additional improvements to the overall study conditions and execution, layout, and human-donor count could be made. To that end, we have
T Eric, Ballard +7 more
openaire +2 more sources
Environment International, 2020 The renal and hepatic clearance rates of organophosphate esters (OPEs) in humans were estimated. Six OPEs and their corresponding diester metabolites (mOPEs) were quantified respectively in 30 paired human plasma and urine samples collected in Hengshui ...
Xiaolei Wang +6 more
doaj +1 more source
Metabolic stability and its role in the discovery of new chemical entities
Acta Pharmaceutica, 2019 Determination of metabolic profiles of new chemical entities is a key step in the process of drug discovery, since it influences pharmacokinetic characteristics of therapeutic compounds.
Słoczyńska Karolina +6 more
doaj +1 more source
QSARs for estimating intrinsic hepatic clearance of organic chemicals in humans
Environmental Toxicology and Pharmacology, 2016 Quantitative structure-activity relationships (QSARs) were developed to predict the in vitro clearance (CLINT) of xenobiotics metabolised in human hepatocytes (118 compounds) and microsomes (115 compounds). Clearance values were gathered from the scientific literature and multiple linear models were built and validated selecting at most 6 predictors ...
Pirovano, Alessandra +5 more
openaire +4 more sources
Intrinsic TNF/TNFR2 interactions fine-tune the CD8 T cell response to respiratory influenza virus infection in mice. [PDF]
PLoS ONE, 2013 TNF is an important inflammatory mediator and a target for intervention. TNF is produced by many cell types and is involved in innate inflammation as well as adaptive immune responses. CD8 T cells produce TNF and can also respond to TNF.
Michael E Wortzman +2 more
doaj +1 more source
Clinical and Translational Science, 2020 In the development of new drugs, the prediction of metabolite‐to‐parent plasma exposure ratio in humans prior to administration in a clinical study has emerged as an important need.
Ernesto Callegari +2 more
doaj +1 more source
The effect of gene polymorphism on ticagrelor metabolism: an in vitro study of 22 CYP3A4 variants in Chinese Han population [PDF]
PeerJBackground Ticagrelor is a novel oral antiplatelet agent which can selectively inhibit P2Y12 receptor. Bleeding and dyspnea are common adverse reactions of ticagrelor in clinic.
Xiaoxia Hu +3 more
doaj +2 more sources