Document Detail


The effect of risperidone on D-amino acid oxidase activity as a hypothesis for a novel mechanism of action in the treatment of schizophrenia.
MedLine Citation:
PMID:  19329549     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
D-Amino acid oxidase (DAO) has been established to be involved in the oxidation of D-serine, an allosteric activator of the N-methyl-D-aspartate-type glutamate receptor in the brain, and to be associated with the onset of schizophrenia. The effect of risperidone, a benzisoxazole derivative, atypical antischizophrenic drug, on the activity of human DAO was tested using an in-vitro oxygraph system and rat C6, stable C6 transformant cells overexpressing mouse DAO (designated as C6/DAO) and pig kidney epithelial cells (LLC-PK(1)). Risperidone has a hyperbolic mixed-type inhibition, designated as 'partial uncompetitive inhibition effect', with K(i) value of 41 microM on human DAO. Risperidone exhibited a protective effect from D-amino acid induced cell death in both C6/DAO and LLC-PK(1) cells with 10% increase in viability. These data indicate the involvement of DAO activity in D-serine metabolism and also suggest a new mechanism of action to risperidone as antischizophrenic drug.
Authors:
R M Abou El-Magd; H K Park; T Kawazoe; S Iwana; K Ono; S P Chung; M Miyano; K Yorita; T Sakai; K Fukui
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-03-27
Journal Detail:
Title:  Journal of psychopharmacology (Oxford, England)     Volume:  24     ISSN:  1461-7285     ISO Abbreviation:  J. Psychopharmacol. (Oxford)     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-06-17     Completed Date:  2010-09-16     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8907828     Medline TA:  J Psychopharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1055-67     Citation Subset:  IM    
Affiliation:
Division of Enzyme Pathophysiology, The Institute for Enzyme Research, The University of Tokushima, Tokushima, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antipsychotic Agents / pharmacology*,  therapeutic use
Apoenzymes / metabolism
Apoproteins / chemistry
Blotting, Western
Catalysis
Cell Survival / drug effects
Culture Media
D-Amino-Acid Oxidase / antagonists & inhibitors*
Enzyme Inhibitors*
Holoenzymes / metabolism
Humans
Kinetics
LLC-PK1 Cells
Mice
Rats
Receptors, N-Methyl-D-Aspartate / metabolism
Recombinant Proteins / metabolism
Risperidone / pharmacology*,  therapeutic use
Schizophrenia / drug therapy*,  enzymology*
Serine / metabolism
Swine
Chemical
Reg. No./Substance:
0/Antipsychotic Agents; 0/Apoenzymes; 0/Apoproteins; 0/Culture Media; 0/Enzyme Inhibitors; 0/Holoenzymes; 0/Receptors, N-Methyl-D-Aspartate; 0/Recombinant Proteins; 106266-06-2/Risperidone; 56-45-1/Serine; EC 1.4.3.3/D-Amino-Acid Oxidase
Comments/Corrections
Comment In:
J Psychopharmacol. 2010 Jul;24(7):1133-4   [PMID:  19939869 ]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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