4-OH and 4-F derivatives were found to have strong affinity for all six CYP450 proteins under study in the present work. 4-F and 3-NO 2 derivatives could be a suitable lead compound inhibitor to CYP1A2 followed by 4-OH derivatives. 4-OH derivative with significant binding affinity ...
Inhibition of hepatic CYP450 by substrates and inhibitors Results of the incubation with substrate-inhibitor and dual substrates are presented in Tables 4 and 5. In general, TB, CM and DXM had only a limited influence on the biotransformation of other substrates (inhibition <20%). In contrast,...
In addition, no appreciable effect was seen for anti-CYP2D6 and 3A4. The results showed that CYP1A2 and 2C9 were the enzymes which metabolized the TCAS. Figure 2. Metabolic conversion rate of TCAS in human liver microsomes plus inhibitors. Values are presented as M ± SD (n = 3). (...
Medications can impact the CYP450 system in numerous ways. For example, metoprolol is metabolized by the CYP2D6 enzyme, while warfarin [Coumadin] is processed by the CYP1A2, CYP2D6, and CYP3A4 enzymes [13]. Inhibitors impede the metabolic activity of one or more CYP450 enzymes. Depending ...