More potent inhibition of human CYP2A6 than mouse CYP2A5 enzyme activities by derivatives of phenylethylamine and benzaldehyde
1. A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. 2. The method was used to test inhibition of human and mouse CYP2A enzymes by three phenylethylamine derivatives 2- (p -tolyl)-ethylamine, amphetamine, 2-phenylethylamine...
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Published in | Xenobiotica Vol. 33; no. 5; pp. 529 - 539 |
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Format | Journal Article |
Language | English |
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01.05.2003
Taylor & Francis |
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Abstract | 1. A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. 2. The method was used to test inhibition of human and mouse CYP2A enzymes by three phenylethylamine derivatives 2- (p -tolyl)-ethylamine, amphetamine, 2-phenylethylamine and benzaldehyde, and two of its derivatives, 4-methylbenzaldehyde and 4-methoxybenzaldehyde. 3. The benzaldehyde derivatives were more potent inhibitors of CYP2A5 than the phenylethylamines. The K ic value of 4-methylbenzaldehyde was 3.4 µ M and for 4-methoxybenzaldehyde it was 0.86 µ M for CYP2A5. 4. Amphetamine is a weak inhibitor of CYP2A6, whereas benzaldehyde is a suicide inhibitor with K inact = 0.16 min − 1 and K I = 18 µ M. The K ic values of 2-phenylethylamine, 2- (p -tolyl)-ethylamine, 4-methylbenzaldehyde and 4-methoxybenzaldehyde were 1.13, 0.23, 0.36 and 0.73 µ M for CYP2A6, respectively. 5. Novel potent inhibitors were found for CYP2A6 and, except for 4-methoxybenzaldehyde, all the compounds inhibited CYP2A5 and CYP2A6 enzymes differentially. These data add to the refinement of CYP2A enzyme active sites and provide chemical leads for developing novel chemical inhibitors of the CYP2A6 enzyme. |
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AbstractList | A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. The method was used to test inhibition of human and mouse CYP2A enzymes by three phenylethylamine derivatives 2-(p-tolyl)-ethylamine, amphetamine, 2-phenylethylamine and benzaldehyde, and two of its derivatives, 4-methylbenzaldehyde and 4-methoxybenzaldehyde. The benzaldehyde derivatives were more potent inhibitors of CYP2A5 than the phenylethylamines. The K sub(ic) value of 4-methylbenzaldehyde was 3.4 mu M and for 4-methoxybenzaldehyde it was 0.86 mu M for CYP2A5. Amphetamine is a weak inhibitor of CYP2A6, whereas benzaldehyde is a suicide inhibitor with K sub(inact) = 0.16 min super(m1) and K sub(l) = 18 mu M. The K sub(ic) values of 2-phenylethylamine, 2-(p-tolyl)-ethylamine, 4-methylbenzaldehyde and 4-methoxybenzaldehyde were 1.13, 0.23, 0.36 and 0.73 mu M for CYP2A6, respectively. Novel potent inhibitors were found for CYP2A6 and, except for 4-methoxybenzaldehyde, all the compounds inhibited CYP2A5 and CYP2A6 enzymes differentially. These data add to the refinement of CYP2A enzyme active sites and provide chemical leads for developing novel chemical inhibitors of the CYP2A6 enzyme. 1. A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. 2. The method was used to test inhibition of human and mouse CYP2A enzymes by three phenylethylamine derivatives 2-(p-tolyl)-ethylamine, amphetamine, 2-phenylethylamine and benzaldehyde, and two of its derivatives, 4-methylbenzaldehyde and 4-methoxybenzaldehyde. 3. The benzaldehyde derivatives were more potent inhibitors of CYP2A5 than the phenylethylamines. The K(ic) value of 4-methylbenzaldehyde was 3.4 micro M and for 4-methoxybenzaldehyde it was 0.86 micro M for CYP2A5. 4. Amphetamine is a weak inhibitor of CYP2A6, whereas benzaldehyde is a suicide inhibitor with K(inact) = 0.16 min(-1) and K(I) = 18 micro M. The K(ic) values of 2-phenylethylamine, 2-(p-tolyl)-ethylamine, 4-methylbenzaldehyde and 4-methoxybenzaldehyde were 1.13, 0.23, 0.36 and 0.73 micro M for CYP2A6, respectively. 5. Novel potent inhibitors were found for CYP2A6 and, except for 4-methoxybenzaldehyde, all the compounds inhibited CYP2A5 and CYP2A6 enzymes differentially. These data add to the refinement of CYP2A enzyme active sites and provide chemical leads for developing novel chemical inhibitors of the CYP2A6 enzyme. 1. A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. 2. The method was used to test inhibition of human and mouse CYP2A enzymes by three phenylethylamine derivatives 2- (p -tolyl)-ethylamine, amphetamine, 2-phenylethylamine and benzaldehyde, and two of its derivatives, 4-methylbenzaldehyde and 4-methoxybenzaldehyde. 3. The benzaldehyde derivatives were more potent inhibitors of CYP2A5 than the phenylethylamines. The K ic value of 4-methylbenzaldehyde was 3.4 µ M and for 4-methoxybenzaldehyde it was 0.86 µ M for CYP2A5. 4. Amphetamine is a weak inhibitor of CYP2A6, whereas benzaldehyde is a suicide inhibitor with K inact = 0.16 min − 1 and K I = 18 µ M. The K ic values of 2-phenylethylamine, 2- (p -tolyl)-ethylamine, 4-methylbenzaldehyde and 4-methoxybenzaldehyde were 1.13, 0.23, 0.36 and 0.73 µ M for CYP2A6, respectively. 5. Novel potent inhibitors were found for CYP2A6 and, except for 4-methoxybenzaldehyde, all the compounds inhibited CYP2A5 and CYP2A6 enzymes differentially. These data add to the refinement of CYP2A enzyme active sites and provide chemical leads for developing novel chemical inhibitors of the CYP2A6 enzyme. |
Author | Raunio, H. Rahnasto, M. Poso, A. Juvonen, R. O. |
Author_xml | – sequence: 1 givenname: M. surname: Rahnasto fullname: Rahnasto, M. organization: Department of Pharmacology and Toxicology, University of Kuopio, POB 1627, 70211 Kuopio, Finland – sequence: 2 givenname: H. surname: Raunio fullname: Raunio, H. organization: Department of Pharmacology and Toxicology, University of Kuopio, POB 1627, 70211 Kuopio, Finland – sequence: 3 givenname: A. surname: Poso fullname: Poso, A. organization: Department of Pharmacology and Toxicology, University of Kuopio, POB 1627, 70211 Kuopio, Finland – sequence: 4 givenname: R. O. surname: Juvonen fullname: Juvonen, R. O. organization: Department of Pharmacology and Toxicology, University of Kuopio, POB 1627, 70211 Kuopio, Finland |
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Keywords | Human Vertebrata Mammalia Mouse Animal Coumarine derivatives Cytochrome P450 Liver Rodentia Benzaldehyde Enzyme inhibitor In vitro |
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Snippet | 1. A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. 2. The method was used to test... A rapid 96-well plate assay method was developed and validated to measure liver microsomal coumarin 7-hydroxylation in vitro. The method was used to test... |
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SubjectTerms | Analytical, structural and metabolic biochemistry Animals Aryl Hydrocarbon Hydroxylases - antagonists & inhibitors Benzaldehydes - chemistry Benzaldehydes - pharmacology Binding, Competitive Biological and medical sciences Cytochrome P-450 CYP2A6 Cytochrome P450 Family 2 Dose-Response Relationship, Drug Enzyme Inhibitors - pharmacology Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Humans Inhibitory Concentration 50 Kinetics Mice Microsomes, Liver - enzymology Mixed Function Oxygenases - antagonists & inhibitors Oxidoreductases Phenethylamines - chemistry Phenethylamines - pharmacology Regression Analysis Structure-Activity Relationship |
Title | More potent inhibition of human CYP2A6 than mouse CYP2A5 enzyme activities by derivatives of phenylethylamine and benzaldehyde |
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