Journal ArticleDOI
Esterase Activities in the Blood, Liver and Intestine of Several Preclinical Species and Humans
TLDR
Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human, and such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.Abstract:
Species and tissue differences in the activity of three major classes of esterases, carboxylesterase (CE), butyrylcholinesterase (BChE) and paraoxonase (PON), were studied. Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human. Such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.read more
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ω-Imidazolyl- and ω-Tetrazolylalkylcarbamates as Inhibitors of Fatty Acid Amide Hydrolase: Biological Activity and in vitro Metabolic Stability
TL;DR: With the aid of esterase inhibitors it was shown that in porcine plasma, carboxylesterase‐like enzymes and paraoxonase are involved in carbamate cleavage, and it was found that highly active pyridin‐3‐yl carbamates reacted with albumin, which led to covalent albumin adducts.
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Physiologically based kinetic modelling based prediction of in vivo rat and human acetylcholinesterase (AChE) inhibition upon exposure to diazinon
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Synthesis of New Branched 2-Nitroimidazole as a Hypoxia Sensitive Linker for Ligand-Targeted Drugs of Paclitaxel
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Journal ArticleDOI
Metabolic Stability and Metabolite Characterization of Capilliposide B and Capilliposide C by LC⁻QTRAP⁻MS/MS.
Zhongzhe Cheng,Xing Zhou,Zhifeng Du,Wenyi Li,Bingying Hu,Jingkui Tian,Lin Zhang,Jiangeng Huang,Hongliang Jiang +8 more
TL;DR: The results updated the preclinical metabolism and disposition process of LC-B and LC-C, which provided additional information for better understanding efficacy and safety, and the metabolic pathway in mice was proposed.
Journal ArticleDOI
Characterization of water-soluble esters of nitrobenzoxadiazole-based GSTP1-1 inhibitors for cancer treatment.
Veronica Di Paolo,Chiara Fulci,Dante Rotili,Anastasia De Luca,Stefano Tomassi,Massimo Serra,Manuel Scimeca,Cristina Geroni,Luigi Quintieri,Anna Maria Caccuri +9 more
TL;DR: Results suggest the possible utility of phosphates 4 and 5 as single agents and in combination regimens in cancers with unmet medical need, including melanoma.