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Molecular Pharmacology

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Research ArticleORIGINAL ARTICLE

Developmental Regulation of β-Carboline-Induced Inhibition of Glycine-Evoked Responses Depends on Glycine Receptor β Subunit Expression

Jean-Marie Mangin, Laurent Nguyen, Catherine Gougnard, Grégory Hans, Bernard Rogister, Shibeshih Belachew, Gustave Moonen, Pascal Legendre and Jean-Michel Rigo
Molecular Pharmacology May 2005, 67 (5) 1783-1796; DOI: https://doi.org/10.1124/mol.104.007435
Jean-Marie Mangin
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Laurent Nguyen
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Catherine Gougnard
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Grégory Hans
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Bernard Rogister
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Shibeshih Belachew
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Gustave Moonen
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Pascal Legendre
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Jean-Michel Rigo
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Abstract

In this work, we show that β-carbolines, which are known negative allosteric modulators of GABAA receptors, inhibit glycine-induced currents of embryonic mouse spinal cord and hippocampal neurons. In both cell types, β-carboline-induced inhibition of glycine receptor (GlyR)-mediated responses decreases with time in culture. Single-channel recordings show that the major conductance levels of GlyR unitary currents shifts from high levels (≥50 pS) in 2 to 3 days in vitro (DIV) neurons to low levels (<50 pS) in 11 to 14 DIV neurons, assessing the replacement of functional homomeric GlyR by heteromeric GlyR. In cultured spinal cord neurons, the disappearance of β-carboline inhibition of glycine responses and high conductance levels is almost complete in mature neurons, whereas a weaker decrease in β-carboline-evoked glycine response inhibition and high conductance level proportion is observed in hippocampal neurons. To confirm the hypothesis that the decreased sensitivity of GlyR to β-carbolines depends on β subunit expression, Chinese hamster ovary cells were permanently transfected either with GlyR α2 subunit alone or in combination with GlyR β subunit. Single-channel recordings revealed that the major conductance levels shifted from high levels (≥50 pS) in GlyR-α2-transfected cells to low levels (<50 pS) in GlyR-α2+β-containing cells. Consistently, both picrotoxin- and β-carboline-induced inhibition of glycine-gated currents were significantly decreased in GlyR-α2+β-transfected cells compared with GlyR-α2-containing cells. In summary, we demonstrate that the incorporation of β subunits in GlyRs confers resistance not only to picrotoxin but also to β-carboline-induced inhibition. Furthermore, we also provide evidence that hippocampal neurons undergo in vitro a partial maturation process of their GlyR-mediated responses.

  • Received September 21, 2004.
  • Accepted February 16, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 67 (5)
Molecular Pharmacology
Vol. 67, Issue 5
1 May 2005
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Research ArticleORIGINAL ARTICLE

Developmental Regulation of β-Carboline-Induced Inhibition of Glycine-Evoked Responses Depends on Glycine Receptor β Subunit Expression

Jean-Marie Mangin, Laurent Nguyen, Catherine Gougnard, Grégory Hans, Bernard Rogister, Shibeshih Belachew, Gustave Moonen, Pascal Legendre and Jean-Michel Rigo
Molecular Pharmacology May 1, 2005, 67 (5) 1783-1796; DOI: https://doi.org/10.1124/mol.104.007435

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Research ArticleORIGINAL ARTICLE

Developmental Regulation of β-Carboline-Induced Inhibition of Glycine-Evoked Responses Depends on Glycine Receptor β Subunit Expression

Jean-Marie Mangin, Laurent Nguyen, Catherine Gougnard, Grégory Hans, Bernard Rogister, Shibeshih Belachew, Gustave Moonen, Pascal Legendre and Jean-Michel Rigo
Molecular Pharmacology May 1, 2005, 67 (5) 1783-1796; DOI: https://doi.org/10.1124/mol.104.007435
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