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.
Keywords: NAT2, acetylation, polymorphism, pharmacogenomics
Drug Metabolism Letters
Title: Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam
Volume: 1 Issue: 1
Author(s): M. Olivera, C. Martinez, G. Gervasini, J. A. Carrillo, S. Ramos, J. Benitez, E. Garcia-Martin and J. A. G. Agundez
Affiliation:
Keywords: NAT2, acetylation, polymorphism, pharmacogenomics
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.
Export Options
About this article
Cite this article as:
Olivera M., Martinez C., Gervasini G., Carrillo A. J., Ramos S., Benitez J., Garcia-Martin E. and G. Agundez A. J., Effect of Common NAT2 Variant Alleles in the Acetylation of the Major Clonazepam Metabolite, 7-minoclonazepam, Drug Metabolism Letters 2007; 1 (1) . https://dx.doi.org/10.2174/187231207779814283
DOI https://dx.doi.org/10.2174/187231207779814283 |
Print ISSN 1872-3128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1874-0758 |
Related Articles
-
Computational Tools in the Discovery of New G-Quadruplex Ligands with Potential Anticancer Activity
Current Topics in Medicinal Chemistry Naturally Occurring and Synthetic Peptides Acting on Nicotinic Acetylcholine Receptors
Current Pharmaceutical Design Overexpression of miR-26a-5p Suppresses Tau Phosphorylation and Aβ Accumulation in the Alzheimer’s Disease Mice by Targeting DYRK1A
Current Neurovascular Research An Enriched Population of CD45, CD34 and CD117 Stem Cells in Human Umbilical Cord Blood for Potential Therapeutic Regenerative Strategies
Current Neurovascular Research Role of Antioxidants in Redox Regulation of Diabetic Cardiovascular Complications
Current Pharmaceutical Biotechnology Targeting Cancer and Neuropathy with Histone Deacetylase Inhibitors:Two Birds with One Stone?
Current Cancer Drug Targets Is Preoperative Endoscopic Biliary Drainage Indicated for Jaundiced Patients with Resectable Pancreatic Cancer?
Current Drug Targets Isothermal Calorimetry Study of the Interactions of Type I Antifreeze Proteins with a Lipid Model Membrane
Protein & Peptide Letters PDE3 Inhibition by Cilostazol Ameliorated Behavioral and Biochemical Deficits in Prenatal Alcohol Induced Experimental ADHD
Current Enzyme Inhibition Promoting Well-being and Resilience in Employing a Relationship Centered Approach: A Case Study of a Pre-adolescent Boy
Adolescent Psychiatry Radionuclide Imaging in Drug Development
Current Pharmaceutical Design Neurogenomic Pathway of Autism Spectrum Disorders: Linking Germline and Somatic Mutations to Genetic-Environmental Interactions
Current Bioinformatics Association of Neutrophil-Lymphocyte Ratio with Mild Cognitive Impairment in Elderly Chinese Adults: A Case-control Study
Current Alzheimer Research Multiple Sclerosis – Established and Novel Therapeutic Approaches
Central Nervous System Agents in Medicinal Chemistry Review of the Phytochemistry and Pharmacological Properties of Valeriana officinalis
Current Traditional Medicine Tuning the Electronic Properties by Width and Length Modifications of Narrow- Diameter Carbon Nanotubes for Nanomedicine
Current Medicinal Chemistry Upregulation of Suppressor of Cytokine Signaling 3 in Microglia by Cinnamic Acid
Current Alzheimer Research Ketamine Induces Toxicity in Human Neurons Differentiated from Embryonic Stem Cells via Mitochondrial Apoptosis Pathway
Current Drug Safety Neuropathological Correlates of Cerebral Multimorbidity
Current Alzheimer Research Editorial (Hot Topic: Palmitoylethanolamide: Biochemistry, Pharmacology and Therapeutic Use of a Pleiotropic Anti-Inflammatory Lipid Mediator)
CNS & Neurological Disorders - Drug Targets