[3H]Thienylcyclohexylpiperidine Binding Activity in Brain Synaptic Membranes Treated with Triton X‐100

Kiyokazu Ogita, Toshitaka Nabeshima, Yukio Yoneda

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Abstract: Binding activity of [3H]thienylcyclohexylpiperidine was examined using rat brain synaptic membranes treated with Triton X‐100. This compound is proposed to be a noncompetitive antagonist for the N‐methyl‐d‐aspartate (NMDA)‐sensitive subclass of brain excitatory amino acid receptors. The activity decreased in proportion to increasing concentrations of the detergent up to 0.08%. In vitro addition of l‐glutamate (Glu) partially restored the decreased activity caused by this Triton treatment, whereas further addition of glycine (Gly) entirely reversed the loss of activity to the level found in membranes extensively washed but not treated with a detergent. These stimulatory effects were found to be due to the acceleration of the association of ligand. The rank order of potentiation of the activity coincided well with that of the affinity for the NMDA‐sensitive subclass among numerous Glu analogs. The potentiation by Gly as well as Glu was invariably prevented by competitive NMDA antagonists, such as dl‐2‐amino‐5‐phosphonovalerate and (×)‐3‐(2‐carboxypiperazin‐4‐yl)propyl‐1‐phosphonate, but not by strychnine. No significant difference was observed between pharmacological profiles of the activities in synaptic membranes treated and not treated with Triton X‐100, except haloperidol. The potency of this σ‐ligand to inhibit the activity was greatly reduced by the Triton treatment in the presence of both Glu and Gly. These results suggest that the regulatory properties of Triton‐treated synaptic membranes remain unchanged in terms of the interaction within the NMDA receptor complex.

Original languageEnglish
Pages (from-to)1639-1646
Number of pages8
JournalJournal of Neurochemistry
Volume55
Issue number5
DOIs
Publication statusPublished - 01-01-1990
Externally publishedYes

Fingerprint

tenocyclidine
Synaptic Membranes
Octoxynol
Glycine
Brain
Membranes
Detergents
Ligands
Strychnine
Glutamate Receptors
Haloperidol
Pharmacology
Rats

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Cellular and Molecular Neuroscience

Cite this

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title = "[3H]Thienylcyclohexylpiperidine Binding Activity in Brain Synaptic Membranes Treated with Triton X‐100",
abstract = "Abstract: Binding activity of [3H]thienylcyclohexylpiperidine was examined using rat brain synaptic membranes treated with Triton X‐100. This compound is proposed to be a noncompetitive antagonist for the N‐methyl‐d‐aspartate (NMDA)‐sensitive subclass of brain excitatory amino acid receptors. The activity decreased in proportion to increasing concentrations of the detergent up to 0.08{\%}. In vitro addition of l‐glutamate (Glu) partially restored the decreased activity caused by this Triton treatment, whereas further addition of glycine (Gly) entirely reversed the loss of activity to the level found in membranes extensively washed but not treated with a detergent. These stimulatory effects were found to be due to the acceleration of the association of ligand. The rank order of potentiation of the activity coincided well with that of the affinity for the NMDA‐sensitive subclass among numerous Glu analogs. The potentiation by Gly as well as Glu was invariably prevented by competitive NMDA antagonists, such as dl‐2‐amino‐5‐phosphonovalerate and (×)‐3‐(2‐carboxypiperazin‐4‐yl)propyl‐1‐phosphonate, but not by strychnine. No significant difference was observed between pharmacological profiles of the activities in synaptic membranes treated and not treated with Triton X‐100, except haloperidol. The potency of this σ‐ligand to inhibit the activity was greatly reduced by the Triton treatment in the presence of both Glu and Gly. These results suggest that the regulatory properties of Triton‐treated synaptic membranes remain unchanged in terms of the interaction within the NMDA receptor complex.",
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[3H]Thienylcyclohexylpiperidine Binding Activity in Brain Synaptic Membranes Treated with Triton X‐100. / Ogita, Kiyokazu; Nabeshima, Toshitaka; Yoneda, Yukio.

In: Journal of Neurochemistry, Vol. 55, No. 5, 01.01.1990, p. 1639-1646.

Research output: Contribution to journalArticle

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T1 - [3H]Thienylcyclohexylpiperidine Binding Activity in Brain Synaptic Membranes Treated with Triton X‐100

AU - Ogita, Kiyokazu

AU - Nabeshima, Toshitaka

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AB - Abstract: Binding activity of [3H]thienylcyclohexylpiperidine was examined using rat brain synaptic membranes treated with Triton X‐100. This compound is proposed to be a noncompetitive antagonist for the N‐methyl‐d‐aspartate (NMDA)‐sensitive subclass of brain excitatory amino acid receptors. The activity decreased in proportion to increasing concentrations of the detergent up to 0.08%. In vitro addition of l‐glutamate (Glu) partially restored the decreased activity caused by this Triton treatment, whereas further addition of glycine (Gly) entirely reversed the loss of activity to the level found in membranes extensively washed but not treated with a detergent. These stimulatory effects were found to be due to the acceleration of the association of ligand. The rank order of potentiation of the activity coincided well with that of the affinity for the NMDA‐sensitive subclass among numerous Glu analogs. The potentiation by Gly as well as Glu was invariably prevented by competitive NMDA antagonists, such as dl‐2‐amino‐5‐phosphonovalerate and (×)‐3‐(2‐carboxypiperazin‐4‐yl)propyl‐1‐phosphonate, but not by strychnine. No significant difference was observed between pharmacological profiles of the activities in synaptic membranes treated and not treated with Triton X‐100, except haloperidol. The potency of this σ‐ligand to inhibit the activity was greatly reduced by the Triton treatment in the presence of both Glu and Gly. These results suggest that the regulatory properties of Triton‐treated synaptic membranes remain unchanged in terms of the interaction within the NMDA receptor complex.

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