A Study on the Mechanism of Inhibition of Human P450 2D6 by Schering 66712 Using Metabolite and 3D Modeling Studies
Diffenderfer, Laura E.
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The P450 enzymes are extremely important for human metabolism of both endogenous and exogenous compounds in the body, especially medicinal drugs. The inhibition of these enzymes by pharmaceuticals can lead to adverse drug reactions if drug levels build up to toxic levels. P450 2D6 is the second leading drug metabolizer of the P450 family and its inhibition by 5- fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine (Schering 66712) was studied here via LC-MS and metabolite studies with P450 2D6, P450 3A4, P450 2C19, and P450 2C9. The P450s were assayed with SCH 66712 and ran on an LC-MS to look for potential metabolites. Only P450 2C9 showed an expected metabolite mass; the others did not show any hypothesized metabolites. Additionally, modeling studies with P450 2D6, P450 3A4 and P450 2C9 were conducted to compare substrate orientation and key amino acid moieties that may be involved in binding and inhibition.
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