Selective effects of alcohols on gamma-aminobutyric acid A receptor subunits expressed in human embryonic kidney cells

J Pharmacol Exp Ther. 1994 Apr;269(1):157-63.

Abstract

Several previous studies implicated alpha 6 and gamma 2L subunits as potential determinants of gamma-aminobutyric acid A (GABAA) receptor channel sensitivity to alcohol modulation. The effects of ethanol and n-octanol were studied on GABA-induced currents in human embryonic kidney cells transfected to express one of three different GABAA receptor channel subunit combinations: alpha 1 beta 2 gamma 2S, alpha 6 beta 2 gamma 2S or alpha 6 beta 2 gamma 2L. No increase in the current amplitude of any subunit combination was observed after the coapplication of GABA and physiological concentrations (10-100 mM) of ethanol. By contrast, the coapplication of GABA and 100 microM octanol increased the current amplitude by 50% to 100% in all three subunit combinations. Octanol produced a shift of the current dose-response curve toward lower concentrations of GABA. Ethanol was effective in increasing the rate of desensitization produced by higher concentrations of GABA in the alpha 6 beta 2 gamma 2S cells but not the alpha 1 beta 2 gamma 2S combination. This ethanol-induced modification of desensitization was not altered by the presence of the protein kinase inhibitor 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H-7). These experiments indicate that the presence of alpha 6 or gamma 2L subunits, in itself, does not result in the potentiation of GABA-induced currents by ethanol, as described in some reports. However, the presence of either the alpha 6 or alpha 1 subunit may determine whether the desensitization rate of the GABAA current is affected by the alcohol.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • 1-Octanol
  • Base Sequence
  • Cell Line
  • Depression, Chemical
  • Embryo, Mammalian / cytology
  • Ethanol / pharmacology*
  • Humans
  • Ion Channels / physiology
  • Isoquinolines / pharmacology
  • Kidney / drug effects*
  • Kidney / embryology
  • Kidney / ultrastructure*
  • Kinetics
  • Macromolecular Substances
  • Molecular Sequence Data
  • Octanols / pharmacology*
  • Piperazines / pharmacology
  • Protein Kinase Inhibitors
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-A / genetics
  • Sensitivity and Specificity
  • Transfection
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / physiology

Substances

  • Ion Channels
  • Isoquinolines
  • Macromolecular Substances
  • Octanols
  • Piperazines
  • Protein Kinase Inhibitors
  • Receptors, GABA-A
  • Ethanol
  • gamma-Aminobutyric Acid
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • 1-Octanol