Allosteric modulation of glycine receptors is more efficacious for partial rather than full agonists

Tímea Bíró, G. Maksay

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Allosteric modulation of [3H]strychnine binding to glycine receptors (GlyRs) was examined in synaptosomal membranes of rat spinal cord. An allosteric model enabled us to determine the cooperativity factors of the allosteric agents with [3H]strychnine and glycine bindings (α and β, respectively). We modified the allosteric model with a slope factor because the slope values of the displacement curves of partial agonists (β-alanine, taurine and γ-aminobutyric acid) were beyond unity. The slope factor was reduced only by 100μM propofol. Further, propofol showed positive cooperativity (β3H]strychnine binding. Displacement by taurine is attenuated by granisetron and m-chlorophenylbiguanide representing negative cooperativity (β≫1) greater than with glycine. The results suggest a developmental role of elevated perinatal levels of taurine and neurosteroids as well as a better allosteric modulation of decreased agonist efficacies for impaired glycine receptor-ionophores.

Original languageEnglish
Pages (from-to)521-527
Number of pages7
JournalNeurochemistry International
Volume44
Issue number7
DOIs
Publication statusPublished - Jun 2004

Fingerprint

Glycine Receptors
Strychnine
Taurine
Propofol
Glycine
Granisetron
Aminobutyrates
Ionophores
Alanine
Neurotransmitter Agents
Spinal Cord
Membranes

Keywords

  • [H]strychnine binding
  • Allosteric model
  • Glycine receptor
  • Partial agonists
  • Propofol
  • Taurine

ASJC Scopus subject areas

  • Cell Biology
  • Molecular Biology
  • Cellular and Molecular Neuroscience

Cite this

Allosteric modulation of glycine receptors is more efficacious for partial rather than full agonists. / Bíró, Tímea; Maksay, G.

In: Neurochemistry International, Vol. 44, No. 7, 06.2004, p. 521-527.

Research output: Contribution to journalArticle

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