Chemistry can be defined as the study of matter and the changes it undergoes. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 7507-86-0, Name is 2-Bromo-5-methoxybenzaldehyde, molecular formula is , belongs to phthalazine compound. In a document, author is Takaoka, Naoki, Name: 2-Bromo-5-methoxybenzaldehyde.
Inhibitory effects of drugs on the metabolic activity of mouse and human aldehyde oxidases and influence on drug-drug interactions
As aldehyde oxidase (AOX) plays an emerging role in drug metabolism, understanding its significance for drug-drug interactions (DDI) is important. Therefore, we tested 10 compounds for species-specific and substrate-dependent differences in the inhibitory effect of AOX activity using genetically engineered HEK293 cells over- expressing human AOX1, mouse AOX1 or mouse AOX3 The IC50 values of 10 potential inhibitors of the three AOX enzymes were determined using phthalazine and O-6-benzylguanine as substrates 17 beta-Estradiol, mena dione, norharmane and raloxifene exhibited marked differences in inhibitory effects between the human and mouse AOX isoforms when the phthalazine substrate was used. Some of the compounds tested exhibited substrate dependent differences m their inhibitory effects. Docking simulations with human AOX1 and mouse AOX3 were conducted for six representative inhibitors. The rank order of the minimum binding energy reflected the order of the corresponding IC50 values. We also evaluated the potential DDI between an AOX substrate (O-6-benzylguanine) and an inhibitor (hydralazine) using chimeric mice with humanized livers. Pretreatment of hydralazine increased the maximum plasma concentration (C-max) and the area under the plasma concentration- time curve (AUC(0-24)) of O-6-benzylguanine compared to single administration. Our in vitro data indicate species-specific and substrate-dependent differences in the inhibitory effects on AOX activity. Our in vivo data demon strate the existence of a DDI which may be of relevance in the clinical context.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 7507-86-0, in my other articles. Name: 2-Bromo-5-methoxybenzaldehyde.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem