[3H]ATPA: a high affinity ligand for GluR5 kainate receptors.
Neuropharmacology
; 38(12): 1811-7, 1999 Dec.
Article
em En
| MEDLINE
| ID: mdl-10608276
ABSTRACT
The pharmacological properties of [3H]ATPA ((RS)-2-amino-3(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid) are described. ATPA is a tert-butyl analogue of AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid) that has been shown to possess high affinity for the GluR5 subunit of kainate receptors. [3H]ATPA exhibits saturable, high affinity binding to membranes expressing human GluR5 (GluR5) kainate receptors (Kd approximately 13 nM). No specific binding was observed in membranes expressing GluR2 and GluR6 receptors. Several compounds known to interact with the GluR5 kainate receptor inhibited [3H]ATPA binding with potencies similar to those obtained for competition of [3H]kainate binding to GluR5. Saturable, high affinity [3H]ATPA binding (Kd approximately 4 nM) was also observed in DRG neuron (DRG) membranes isolated from neonatal rats. The rank order potency of compounds to inhibit [3H]ATPA binding in rat DRG and GluR5 membranes were in agreement. These finding demonstrate that [3H]ATPA can be used as a radioligand to examine the pharmacological properties of GluR5 containing kainate receptors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Propionatos
/
Receptores de Ácido Caínico
/
Agonistas de Aminoácidos Excitatórios
/
Gânglios Espinais
/
Isoxazóis
/
Ácido Caínico
/
Neurônios
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Neuropharmacology
Ano de publicação:
1999
Tipo de documento:
Article
País de afiliação:
Canadá