Kinetic cooperative effect of glycine receptor agonists and antagonists on the dissociation of strychnine binding

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Abstract

The dissociation of [3H]strychnine binding was studied in synaptosomal membranes of rat spinal cord. Dissociation elicited by 100-fold dilution was accelerated by completely displacing concentrations of glycinergic agents. The rank order of acceleration was iso-THAZ <strychnine ≈ taurine <R 5135 <avermectin b1a ≈ β-alanine ≪ glycine (THAZ, 5,6,7,8-tetrahydro-4H-isoxazolo-(3,4-d) azepin-3-ol). the accelerating effects were correlated with the changes of entropy (r = 0.93) but not with the changes of free energies (r = 0.06) of their binding. Half-maximal acceleration was elicited by 58 μM glycine. The accelerating effects of glycine and β-alanine were attenuated by the antagonists.

Original languageEnglish
Pages (from-to)183-185
Number of pages3
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume245
Issue number2
DOIs
Publication statusPublished - Apr 15 1993

Fingerprint

Glycine Receptors
Strychnine
Glycine
RU 5135
Alanine
Glycine Agents
Taurine
Entropy
Spinal Cord
Membranes

Keywords

  • (agonist and antagonist)
  • Entropy change of binding
  • Glycine receptor
  • Kinetic cooperativity of dissociation
  • [H]Strychnine binding

ASJC Scopus subject areas

  • Pharmacology

Cite this

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abstract = "The dissociation of [3H]strychnine binding was studied in synaptosomal membranes of rat spinal cord. Dissociation elicited by 100-fold dilution was accelerated by completely displacing concentrations of glycinergic agents. The rank order of acceleration was iso-THAZ 1a ≈ β-alanine ≪ glycine (THAZ, 5,6,7,8-tetrahydro-4H-isoxazolo-(3,4-d) azepin-3-ol). the accelerating effects were correlated with the changes of entropy (r = 0.93) but not with the changes of free energies (r = 0.06) of their binding. Half-maximal acceleration was elicited by 58 μM glycine. The accelerating effects of glycine and β-alanine were attenuated by the antagonists.",
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AB - The dissociation of [3H]strychnine binding was studied in synaptosomal membranes of rat spinal cord. Dissociation elicited by 100-fold dilution was accelerated by completely displacing concentrations of glycinergic agents. The rank order of acceleration was iso-THAZ 1a ≈ β-alanine ≪ glycine (THAZ, 5,6,7,8-tetrahydro-4H-isoxazolo-(3,4-d) azepin-3-ol). the accelerating effects were correlated with the changes of entropy (r = 0.93) but not with the changes of free energies (r = 0.06) of their binding. Half-maximal acceleration was elicited by 58 μM glycine. The accelerating effects of glycine and β-alanine were attenuated by the antagonists.

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