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National Institute of Environmental Health Sciences

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Publication Detail

Title: Coumarin substrates for cytochrome P450 2D6 fluorescence assays.

Authors: Nakamura, K; Hanna, I H; Cai, H; Nishimura, Y; Williams, K M; Guengerich, F P

Published In Anal Biochem, (2001 May 15)

Abstract: A set of nine 4-aminomethyl-7-alkoxycoumarin derivatives was synthesized and characterized as substrates for O-dealkylation by recombinant cytochrome P450 2D6, a major human enzyme involved in drug metabolism. Enzymatic O-dealkylation yields 7-hydroxycoumarins, which have useful fluorescence properties. The substrates, which differed in substitution at the amino and 7-hydroxy positions, varied in terms of catalytic efficiency of O-dealkylation and in their selectivity as substrates for cytochrome P450 2D6 in human liver microsomes. Several of the compounds are useful as cytochrome P450 2D6 substrates in single-phase, rapid-throughput assays.

PubMed ID: 11355862 Exiting the NIEHS site

MeSH Terms: Amino Acid Sequence; Catalysis/drug effects; Coumarins/chemical synthesis; Coumarins/chemistry*; Coumarins/metabolism*; Cytochrome P-450 CYP2D6/antagonists & inhibitors; Cytochrome P-450 CYP2D6/chemistry; Cytochrome P-450 CYP2D6/isolation & purification; Cytochrome P-450 CYP2D6/metabolism*; Enzyme Inhibitors/pharmacology; Fluorescent Dyes/chemical synthesis; Fluorescent Dyes/chemistry*; Fluorescent Dyes/metabolism*; Humans; Kinetics; Microsomes, Liver/drug effects; Microsomes, Liver/enzymology; Microsomes, Liver/metabolism; Molecular Sequence Data; Quinidine/pharmacology; Recombinant Proteins/antagonists & inhibitors; Recombinant Proteins/chemistry; Recombinant Proteins/isolation & purification; Recombinant Proteins/metabolism; Research Support, U.S. Gov't, P.H.S.; Substrate Specificity

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