Establishment of CHO cell lines expressing four N-methyl-D-aspartate receptor subtypes and characterization of a novel antagonist PPDC.
FEBS Lett
; 506(2): 117-22, 2001 Oct 05.
Article
em En
| MEDLINE
| ID: mdl-11591383
ABSTRACT
To develop an assay system that allows the N-methyl-D-aspartate (NMDA) receptor subtype-selective antagonistic potency of drugs, we have established Chinese hamster ovary cell lines expressing the four NMDA receptor subtypes (GluRepsilon1/zeta1-GluRepsilon4/zeta1) heat-indelibly. Using these clonal cells, we found that a novel antagonist, (1S,2R)-1-phenyl-2[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide, was less selective for the GluRepsilon1/zeta1 the IC(50) values for the GluRepsilon1/zeta1-GluRepsilon4/zeta1 were 41.7, 13.3, 12.6 and 11.5 microM, respectively, while two well-known antagonists, DL-2-amino-5-phosphonovaleric acid and ifenprodil, showed the known potency and selectivity for each subtype. Thus, the established clonal cells are of use in characterizing the pharmacological properties of drugs that act on NMDA receptors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Valina
/
Células CHO
/
Receptores de N-Metil-D-Aspartato
/
Antagonistas de Aminoácidos Excitatórios
/
Ciclopropanos
Limite:
Animals
Idioma:
En
Revista:
FEBS Lett
Ano de publicação:
2001
Tipo de documento:
Article
País de afiliação:
Japão