[125I]thienylphencyclidine, a novel ligand for the NMDA receptor.
Eur J Pharmacol
; 226(1): 53-8, 1992 May 12.
Article
en En
| MEDLINE
| ID: mdl-1356810
ABSTRACT
We have monitored the binding of [125I]thienylphencyclidine ([125I]TCP), a novel high affinity radioiodinated ligand that specifically recognizes the NMDA (N-methyl-D-aspartate) receptor in rat brain membranes. [125I]TCP binds with an affinity of about 30 nM, and recognizes a similar number of binding sites to previously employed ligands for this receptor. [125I]TCP binding is characterized by slow association and dissociation rates, and the latter can be modified by the addition of Mg2+ or Zn2+, as previously described for [3H]dizocilpine ([3H]MK801). Other phencyclidine-like ligands displaced [125I]TCP binding with the order of potency dizocilpine greater than thienylphencyclidine greater than ITCP greater than phencyclidine greater than ketamine. The binding of [125I]TCP was also increased by NMDA and glycine-site agonists and inhibited by antagonists of these sites. Surprisingly, however, the polyamines spermidine and spermine did not increase [125I]TCP, even though the polyamine antagonist arcaine was an effective inhibitor of binding. These results show that [125I]TCP is a useful ligand for the NMDA receptor complex that binds to the receptor in a manner that is qualitatively distinct from previously described ligands.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fenciclidina
/
Encéfalo
/
Receptores de N-Metil-D-Aspartato
Límite:
Animals
Idioma:
En
Revista:
Eur J Pharmacol
Año:
1992
Tipo del documento:
Article