Access

You are not currently logged in.

Access your personal account or get JSTOR access through your library or other institution:

login

Log in to your personal account or through your institution.

Steroid Hormone Metabolites are Barbiturate-Like Modulators of the GABA Receptor

Maria Dorota Majewska, Neil L. Harrison, Rochelle D. Schwartz, Jeffery L. Barker and Steven M. Paul
Science
New Series, Vol. 232, No. 4753 (May 23, 1986), pp. 1004-1007
Stable URL: http://www.jstor.org/stable/1696201
Page Count: 4
  • More info
  • Cite this Item
Steroid Hormone Metabolites are Barbiturate-Like Modulators of the GABA Receptor
Preview not available

Abstract

Two metabolites of the steroid hormones progesterone and deoxycorticosterone, 3α-hydroxy-5α-dihydroprogesterone and 3α,5α-tetrahydrodeoxycorticosterone, are potent barbiturate-like ligands of the γ-aminobutyric acid (GABA) receptor--chloride ion channel complex. At concentrations between 10$^{-7}$ and 10$^{-5}$ M both steroids inhibited binding of the convulsant t-butylbicyclophosphorothionate to the GABA-receptor complex and increased the binding of the benzodiazepine flunitrazepam; they also stimulated chloride uptake (as measured by uptake of $^{36}$Cl$^{-}$) into isolated brain vesicles, and potentiated the inhibitory actions of GABA in cultured rat hippocampal and spinal cord neurons. These data may explain the ability of certain steroid hormones to rapidly alter neuronal excitability and may provide a mechanism for the anesthetic and hypnotic actions of naturally occurring and synthetic anesthetic steroids.

Page Thumbnails

  • Thumbnail: Page 
1004
    1004
  • Thumbnail: Page 
1005
    1005
  • Thumbnail: Page 
1006
    1006
  • Thumbnail: Page 
1007
    1007