Characterization of D-3,4-cyclopropylglutamates as N-methyl-D-aspartate receptor agonists.
Neurosci Lett
; 112(2-3): 328-32, 1990 May 04.
Article
em En
| MEDLINE
| ID: mdl-2163042
ABSTRACT
The 4 configurational isomers of D-3,4-cyclopropylglutamate (D-CGA) have been synthesized and analyzed for their interactions as excitatory amino acid recognition sites. Additionally, functional assessment of the action of these compounds at the N-methyl-D-aspartate (NMDA) receptor was performed. All 4 analogs function as agonists at the NMDA receptor as evidenced by their ability to stimulate [3H]MK-801 binding to the coupled PCP recognition site. Furthermore, the rank order of potency of these compounds in stimulating [3H]MK-801 binding corresponds with their Ki values for the displacement of NMDA-selective L-[3H]glutamate and [3H]CGS-19755 binding (D-CGA-C greater than D-CGA-B greater than D-CGA-D greater than D-CGA-A). The D-CGA-C isomer has affinity and potency at the NMDA receptor similar to the endogenous agonist, L-glutamate. This high potency coupled with greater specificity than L-glutamate, makes D-CGA-C a potentially useful pharmacological tool for the study of this receptor.
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Base de dados:
MEDLINE
Assunto principal:
Receptores de Neurotransmissores
/
Receptores de Superfície Celular
/
Dibenzocicloeptenos
/
Aminoácidos Dicarboxílicos
Idioma:
En
Ano de publicação:
1990
Tipo de documento:
Article