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

Published

Journal Article

A series of short-chain alcohols, including ethanol, were examined for their abilities to stimulate gamma-aminobutyric acid (GABA) receptor-mediated chloride uptake into isolated brain vesicles. All of the alcohols tested stimulated 36 chloride 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 less than 0.0001) and their membrane/buffer partition coefficients (r = 0.91; P less than 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, be mediated via an action at central GABA receptors.

Full Text

Duke Authors

Cited Authors

  • Suzdak, PD; Schwartz, RD; Skolnick, P; Paul, SM

Published Date

  • March 22, 1988

Published In

Volume / Issue

  • 444 / 2

Start / End Page

  • 340 - 345

PubMed ID

  • 2834024

Pubmed Central ID

  • 2834024

International Standard Serial Number (ISSN)

  • 0006-8993

Digital Object Identifier (DOI)

  • 10.1016/0006-8993(88)90943-2

Language

  • eng

Conference Location

  • Netherlands