[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 journalArticle

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

Fingerprint

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 journalArticle

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.
@article{c66a056d3ccd4d0aacb5af5d6e4e6145,
title = "[125I]Thienylphencyclidine, a novel ligand for the NMDA receptor",
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.",
keywords = "NMDA receptor, Polyamines, [I]Thienylphencyclidinc",
author = "Reynolds, {Ian J.} and Kristi Rothermund and Sunita Rajdev and Fauq, {Abdul H.} and Kozikowski, {Alan P.}",
year = "1992",
month = "5",
day = "12",
doi = "10.1016/0922-4106(92)90082-7",
language = "English (US)",
volume = "226",
pages = "53--58",
journal = "European Journal of Pharmacology - Molecular Pharmacology Section",
issn = "0922-4106",
publisher = "Elsevier BV",
number = "1",

}

TY - JOUR

T1 - [125I]Thienylphencyclidine, a novel ligand for the NMDA receptor

AU - Reynolds, Ian J.

AU - Rothermund, Kristi

AU - Rajdev, Sunita

AU - Fauq, Abdul H.

AU - Kozikowski, Alan P.

PY - 1992/5/12

Y1 - 1992/5/12

N2 - 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.

AB - 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.

KW - NMDA receptor

KW - Polyamines

KW - [I]Thienylphencyclidinc

UR - http://www.scopus.com/inward/record.url?scp=0027118148&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0027118148&partnerID=8YFLogxK

U2 - 10.1016/0922-4106(92)90082-7

DO - 10.1016/0922-4106(92)90082-7

M3 - Article

C2 - 1356810

AN - SCOPUS:0027118148

VL - 226

SP - 53

EP - 58

JO - European Journal of Pharmacology - Molecular Pharmacology Section

JF - European Journal of Pharmacology - Molecular Pharmacology Section

SN - 0922-4106

IS - 1

ER -