Allopregnanolone acts as an inhibitory modulator on α1- and α6-containing GABAA receptors

Charlotte A E Hauser*, Christian H R Wetzel, Rainer Rupprecht, Florian Holsboer

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Allopregnanolone, known so far to act as a γ-aminobutyric acid (GABA) agonist, allosterically decreased the affinity of the GABA agonist muscimol for recombinant α1β2γ2 and α6β2γ2 GABAA receptors. Pregnenolone sulfate, a GABA antagonist, had a similar effect. Both of these neuroactive steroids also reduced the time constant of desensitization (τ) of GABA-induced chloride currents. The effect on desensitization was demonstrated for native receptors of hypothalamic neurons as well as for the recombinant GABAA receptors. Hence neuroactive steroids may differentially modulate distinct assemblies of GABAA receptors and thus induce a more subtle modulation of GABAergic synaptic transmission than previously thought possible.

Original languageEnglish (US)
Pages (from-to)531-536
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume219
Issue number2
DOIs
StatePublished - Feb 15 1996
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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