Alcohols stimulate γ-aminobutyric acid receptor-mediated chloride uptake in brain vesicles: correlation with intoxication potency

Peter D. Suzdak, Rochelle D. Schwartz, Phil Skolnick, Steven M. Paul

Research output: Contribution to journalArticlepeer-review

75 Scopus citations

Abstract

A series of short-chain alcohols, including ethanol, were examined for their abilities to stimulate γ-aminobutyric acid (GABA) receptor-mediated chloride uptake into isolated brain vesicles. All of the alcohols tested stimulated 36chloride uptake, at concentrations that occur during acute intoxication, and their potencies in stimulating GABA receptor-mediated chloride uptake were highly correlated with both their intoxication potencies in rats (r = 0.96; P < 0.0001) and their membrane/buffer partition coefficients (r = 0.91; P < 0.0005). Thus, the activity of alcohols at the GABA receptor-coupled chloride ion channel appears to be related to their ability to enter hydrophobic regions of the neuronal membrane. These data suggest that the anxiolytic, sedative/hypnotic and intoxicating properties of ethanol may, in part, in mediated via an action at central GABA receptors.

Original languageEnglish
Pages (from-to)340-345
Number of pages6
JournalBrain Research
Volume444
Issue number2
DOIs
StatePublished - Mar 22 1988

Keywords

  • Alcohol toxicity
  • Brain vesicle
  • Chloride channel
  • Chloride uptake
  • γ-Aminobutyric acid (GABA)

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