Effect of common NAT2 variant alleles in the acetylation of the major clonazepam metabolite, 7-aminoclonazepam

M Olivera; C Martínez; G Gervasini; J A Carrillo; S Ramos; J Benítez; E García-Martin; J A G Agúndez

doi:10.2174/187231207779814283

Effect of common NAT2 variant alleles in the acetylation of the major clonazepam metabolite, 7-aminoclonazepam

Drug Metab Lett. 2007 Jan;1(1):3-5. doi: 10.2174/187231207779814283.

Authors

M Olivera¹, C Martínez, G Gervasini, J A Carrillo, S Ramos, J Benítez, E García-Martin, J A G Agúndez

Affiliation

¹ Department of Pharmacology, Medical School, University of Extremadura, Badajoz, Spain.

PMID: 19356010
DOI: 10.2174/187231207779814283

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetylation
Alleles
Animals
Arylamine N-Acetyltransferase / genetics
Arylamine N-Acetyltransferase / metabolism*
COS Cells
Chlorocebus aethiops
Clonazepam / analogs & derivatives*
Clonazepam / metabolism*
Humans
Pharmacogenetics
Polymorphism, Genetic
Transfection

Substances

7-aminoclonazepam
Clonazepam
Arylamine N-Acetyltransferase
NAT2 protein, human