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TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling.

Publication ,  Journal Article
Bonhaus, DW; McNamara, JO
Published in: Neurosci Biobehav Rev
1989

Findings from numerous pharmacological and electrophysiological studies have uniquely implicated the N-methyl-D-aspartate (NMDA) receptor in kindling. Recent findings indicate that this receptor is regulated by ligands acting at both amino acid (NMDA and glycine) and ion (Zn++ and Mg++) binding sites. To examine the role of the NMDA receptor in kindling it will be necessary to understand how ligands for these different binding sites interact to control activation of the NMDA receptor. To this end we examined a biochemical tool for measuring opening of the NMDA receptor-gated ion channel (NMDA channel). [3H]N-(1-[thienyl] cyclohexyl)piperidine (TCP) binding to brain membranes is stimulated by NMDA and glycine receptor agonists. We have shown that NMDA and glycine increase TCP binding by increasing the access of TCP to its site. Moreover, the pharmacology of the NMDA and glycine binding sites regulating TCP binding is identical to that of the sites regulating NMDA evoked currents. These findings strongly suggest that glycine and NMDA regulate TCP binding by increasing the opening of the NMDA channel. That is NMDA and glycine increase the overall time that the channel is open thereby increasing the time available for TCP to diffuse to its binding site. These findings support the use of TCP binding (association rate) as a marker of channel opening and thereby permit measurement of NMDA receptor activation and ligand binding under identical conditions. This will allow direct testing the hypothesis that an alteration in the NMDA receptor/channel complex itself underlies the increased seizure response of kindled animals.

Duke Scholars

Published In

Neurosci Biobehav Rev

ISSN

0149-7634

Publication Date

1989

Volume

13

Issue

4

Start / End Page

261 / 267

Location

United States

Related Subject Headings

  • Receptors, Neurotransmitter
  • Receptors, N-Methyl-D-Aspartate
  • Phencyclidine
  • N-Methylaspartate
  • Kindling, Neurologic
  • Glycine
  • Brain
  • Behavioral Science & Comparative Psychology
  • Aspartic Acid
  • Animals
 

Citation

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Bonhaus, D. W., & McNamara, J. O. (1989). TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling. Neurosci Biobehav Rev, 13(4), 261–267.
Bonhaus, D. W., and J. O. McNamara. “TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling.Neurosci Biobehav Rev 13, no. 4 (1989): 261–67.
Bonhaus DW, McNamara JO. TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling. Neurosci Biobehav Rev. 1989;13(4):261–7.
Bonhaus, D. W., and J. O. McNamara. “TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling.Neurosci Biobehav Rev, vol. 13, no. 4, 1989, pp. 261–67.
Bonhaus DW, McNamara JO. TCP binding: a tool for studying NMDA receptor-mediated neurotransmission in kindling. Neurosci Biobehav Rev. 1989;13(4):261–267.
Journal cover image

Published In

Neurosci Biobehav Rev

ISSN

0149-7634

Publication Date

1989

Volume

13

Issue

4

Start / End Page

261 / 267

Location

United States

Related Subject Headings

  • Receptors, Neurotransmitter
  • Receptors, N-Methyl-D-Aspartate
  • Phencyclidine
  • N-Methylaspartate
  • Kindling, Neurologic
  • Glycine
  • Brain
  • Behavioral Science & Comparative Psychology
  • Aspartic Acid
  • Animals