Effects on γ-Aminobutyric Acid (GABA)A Receptors of a Neuroactive Steroid That Negatively Modulates Glutamate Neurotransmission and Augments GABA Neurotransmission

Effects on γ-Aminobutyric Acid (GABA)A Receptors of a Neuroactive Steroid That Negatively Modulates Glutamate Neurotransmission and Augments GABA Neurotransmission

Neurosteroids positively and negatively modulate γ-aminobutyric acid (GABA)A receptors and glutamate receptors, which underlie most fast inhibition and excitation in the central nervous system. We report the identification of a neuroactive steroid, (3α,5β)-20-oxo-pregnane-3-carboxylic acid (3α5βPC),...

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Veröffentlicht in:Molecular pharmacology 2001-10, Vol.60 (4), p.732-741
Hauptverfasser: Mennerick, Steven, Zeng, Chun-Min, Benz, Ann, Shen, Weixing, Izumi, Yukitoshi, Evers, Alex S., Covey, Douglas F., Zorumski, Charles F.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Electrophysiology
Hippocampus - drug effects
Hippocampus - metabolism
Hydrogen-Ion Concentration
In Vitro Techniques
Pregnanes - pharmacology
Rats
Receptors, GABA-A - drug effects
Receptors, GABA-A - metabolism
Steroids - pharmacology
Synapses - drug effects
Synapses - metabolism
Xenopus laevis
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Zusammenfassung:Neurosteroids positively and negatively modulate γ-aminobutyric acid (GABA)A receptors and glutamate receptors, which underlie most fast inhibition and excitation in the central nervous system. We report the identification of a neuroactive steroid, (3α,5β)-20-oxo-pregnane-3-carboxylic acid (3α5βPC), with unique cellular actions. 3α5βPC positively modulates GABAA receptor function and negatively modulates N-methyl-d-aspartate (NMDA) receptor function, a combination that may be of particular clinical benefit. 3α5βPC promotes net GABAA potentiation at low steroid concentrations (
ISSN:0026-895X
DOI:10.1016/S0026-895X(24)12300-0