Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam

M. Olivera; C. Martinez; G. Gervasini; J. A. Carrillo; J. A. Carrillo; S. Ramos; J. Benitez; E. Garcia-Martin; J. A. G. Agundez

doi:10.2174/187231207779814283

ISSN: 1872-3128
E-ISSN: 1874-0758

Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam
Authors: M. Olivera¹, C. Martinez², G. Gervasini³, J. A. Carrillo⁴, J. A. Carrillo⁵, S. Ramos⁶, J. Benitez⁷, E. Garcia-Martin⁸ and J. A. G. Agundez⁹
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¹ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ² Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ³ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁴ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁵ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁶ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁷ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁸ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain. ⁹ Departmento de Farmacologia,Facultad de Medicina, Universidad de Extremadura, Avda de Elvas s/n, E-06071, Badajoz, Spain.
Source: Drug Metabolism Letters, Volume 1, Issue 1, Jan 2007, p. 3 - 5
DOI: https://doi.org/10.2174/187231207779814283
- Available online: 01 Jan 2007

Abstract

We investigated the role of NAT2 on clonazepam acetylation, using transiently expressed human NAT2 alleles. The NAT25*B and the NAT2*6A variant alleles cause a 20 and 22-fold reduction in the Vmax, respectively. We conclude that NAT2 is responsible for 7-aminoclonazepam acetylation and that NAT2 gene polymorphisms impair such metabolic pathway.

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2007-01-01

2025-10-20

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Article Type: Research Article

Keyword(s): acetylation; NAT2; pharmacogenomics; polymorphism

Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam

Abstract

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