Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes

AIMS: To study the influence of CYP2D6*10 on the formation of p-hydroxymexiletine (PHM) and hydroxymethylmexiletine (HMM) using microsomes from human liver of known genotypes. METHODS: Microsomes from human livers of genotype CYP2D6*1/*1 (n = 5), *1/*10 (n = 6) and *10/*10 (n = 6) were used in this...

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Prif Awduron: Senda, C, Yamaura, Y, Kobayashi, K, Fujii, H, Minami, H, Sasaki, Y, Igarashi, T, Chiba, K
Fformat: Erthygl
Iaith:English
Cyhoeddwyd: Blackwell Science Inc 2001
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Short Reports
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC2014511/
https://ncbi.nlm.nih.gov/pubmed/11453897
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1046/j.0306-5251.2001.01411.x
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spelling pubmed-20145112008-01-14 Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes Senda, C Yamaura, Y Kobayashi, K Fujii, H Minami, H Sasaki, Y Igarashi, T Chiba, K Br J Clin Pharmacol Short Reports AIMS: To study the influence of CYP2D6*10 on the formation of p-hydroxymexiletine (PHM) and hydroxymethylmexiletine (HMM) using microsomes from human liver of known genotypes. METHODS: Microsomes from human livers of genotype CYP2D6*1/*1 (n = 5), *1/*10 (n = 6) and *10/*10 (n = 6) were used in this study. The formation of PHM and HMM was determined by high-performance liquid chromatography. RESULTS: The formation rates of PHM and HMM were decreased by more than 50% and 85% in CYP2D6*1/*10 and *10/*10 microsomes, respectively, compared with *1/*1 microsomes. CONCLUSIONS: The metabolism of mexiletine to form PHM and HMM appears to be impaired to a significant extent in human liver microsomes from hetero- and homozygotes of CYP2D6*10. Blackwell Science Inc 2001-07 /pmc/articles/PMC2014511/ /pubmed/11453897 http://dx.doi.org/10.1046/j.0306-5251.2001.01411.x Text en © 2001 Blackwell Science Ltd
institution US National Library of Medicine
collection PubMed Central
language English
format Article
topic Short Reports
spellingShingle Short Reports
Senda, C
Yamaura, Y
Kobayashi, K
Fujii, H
Minami, H
Sasaki, Y
Igarashi, T
Chiba, K
Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
description AIMS: To study the influence of CYP2D6*10 on the formation of p-hydroxymexiletine (PHM) and hydroxymethylmexiletine (HMM) using microsomes from human liver of known genotypes. METHODS: Microsomes from human livers of genotype CYP2D6*1/*1 (n = 5), *1/*10 (n = 6) and *10/*10 (n = 6) were used in this study. The formation of PHM and HMM was determined by high-performance liquid chromatography. RESULTS: The formation rates of PHM and HMM were decreased by more than 50% and 85% in CYP2D6*1/*10 and *10/*10 microsomes, respectively, compared with *1/*1 microsomes. CONCLUSIONS: The metabolism of mexiletine to form PHM and HMM appears to be impaired to a significant extent in human liver microsomes from hetero- and homozygotes of CYP2D6*10.
author Senda, C
Yamaura, Y
Kobayashi, K
Fujii, H
Minami, H
Sasaki, Y
Igarashi, T
Chiba, K
author_facet Senda, C
Yamaura, Y
Kobayashi, K
Fujii, H
Minami, H
Sasaki, Y
Igarashi, T
Chiba, K
author_sort Senda, C
title Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
title_short Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
title_full Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
title_fullStr Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
title_full_unstemmed Influence of the CYP2D6*10 allele on the metabolism of mexiletine by human liver microsomes
title_sort influence of the cyp2d6*10 allele on the metabolism of mexiletine by human liver microsomes
publisher Blackwell Science Inc
publisher_facet Blackwell Science Inc
publishDate 2001
url https://ncbi.nlm.nih.gov/pmc/articles/PMC2014511/
https://ncbi.nlm.nih.gov/pubmed/11453897
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1046/j.0306-5251.2001.01411.x
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