[125I]Thienylphencyclidine, a novel ligand for the NMDA receptor

Ian J. Reynolds, Kristi Rothermund, Sunita Rajdev, Abdul H. Fauq, Alan P. Kozikowski

Research output: Contribution to journal › Article

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 ([3MK801). Other phencylidine-like ligands displaced [125I]TCP binding with the order of potency dizocilpine > thienylphencyclidine > ITCP > phencyclidine > 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.

Original languageEnglish (US)
Pages (from-to)53-58
Number of pages6
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume226
Issue number1
DOIs
StatePublished - May 12 1992
Externally publishedYes

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N-Methyl-D-Aspartate Receptors
Ligands
Dizocilpine Maleate
Polyamines
Sarcosine
Phencyclidine
Spermidine
Spermine
Ketamine
N-Methylaspartate
Binding Sites
Membranes
Brain

Keywords

  • NMDA receptor
  • Polyamines
  • [I]Thienylphencyclidinc

ASJC Scopus subject areas

  • Pharmacology
  • Cellular and Molecular Neuroscience

Cite this

[125I]Thienylphencyclidine, a novel ligand for the NMDA receptor. / Reynolds, Ian J.; Rothermund, Kristi; Rajdev, Sunita; Fauq, Abdul H.; Kozikowski, Alan P.

In: European Journal of Pharmacology: Molecular Pharmacology, Vol. 226, No. 1, 12.05.1992, p. 53-58.

Research output: Contribution to journal › Article

Reynolds, IJ, Rothermund, K, Rajdev, S, Fauq, AH & Kozikowski, AP 1992, '[125I]Thienylphencyclidine, a novel ligand for the NMDA receptor', European Journal of Pharmacology: Molecular Pharmacology, vol. 226, no. 1, pp. 53-58. https://doi.org/10.1016/0922-4106(92)90082-7
Reynolds IJ, Rothermund K, Rajdev S, Fauq AH, Kozikowski AP. [125I]Thienylphencyclidine, a novel ligand for the NMDA receptor. European Journal of Pharmacology: Molecular Pharmacology. 1992 May 12;226(1):53-58. https://doi.org/10.1016/0922-4106(92)90082-7
Reynolds, Ian J. ; Rothermund, Kristi ; Rajdev, Sunita ; Fauq, Abdul H. ; Kozikowski, Alan P. / [125I]Thienylphencyclidine, a novel ligand for the NMDA receptor. In: European Journal of Pharmacology: Molecular Pharmacology. 1992 ; Vol. 226, No. 1. pp. 53-58.
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