GABAA receptor modulating steroid antagonists (GAMSA) are functional in vivo.
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TLDR
It is shown that pharmacological treatment with allopregnanolone can promote neurogenesis and positively influence learning and memory of trace eye-blink conditioning in mice and that 3β-hydroxy-steroids antagonize this positive neurosteroid-mediated modulation of the GABAA receptor.About:
This article is published in The Journal of Steroid Biochemistry and Molecular Biology.The article was published on 2016-06-01 and is currently open access. It has received 29 citations till now. The article focuses on the topics: Allopregnanolone & Tetrahydrodeoxycorticosterone.read more
Citations
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GR3027 reversal of neurosteroid-induced, GABA-A receptor-mediated inhibition of human brain function: an allopregnanolone challenge study
Maja Johansson,Maria Månsson,Lars-Eric Lins,Bruce Scharschmidt,Magnus Doverskog,Torbjörn Bäckström,Torbjörn Bäckström +6 more
TL;DR: Oral GR3027 mitigates inhibition of brain function induced by allopregnanolone at doses which are clinically well tolerated and associated with linear pharmacokinetics.
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Neurosteroids Involvement in the Epigenetic Control of Memory Formation and Storage
TL;DR: The epigenetic control of neurosteroids involvement in memory formation and maintenance could represent the basis for neuroregenerative therapies.
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Neurosteroids, GABAA receptors and neurosteroid based drugs: are we witnessing the dawn of the new psychiatric drugs?
Ante Tvrdeić,Ljiljana Poljak +1 more
TL;DR: The purpose of this review paper is to analyze recent research in the field of neurosteroids and neurosteroid-based drugs with emphasis on interaction of Neurosteroids with brain GABAA receptors and the therapeutic potential of GAMS, GAMSA, and TSPO activators.
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New Therapies of Liver Diseases: Hepatic Encephalopathy.
C. Mangini,Sara Montagnese +1 more
TL;DR: A narrative review of HE management strategies can be found in this article, where a small number of new drugs/alternative management strategies have become available, while others are underway, in a pragmatic and hopefully useful fashion.
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Synthesis and antiproliferative activity of 3α‐hydroxyl‐3β‐methoxymethyl‐5α‐pregnan‐20‐one with a C‐21 hydrophilic substituent
TL;DR: Among the compounds, aminosteroid 7 and piperazinyl steroid 14 were most potent against the proliferation of human prostate cancer PC-3 cells with IC50 values of 42 and 82 μmol L−1, respectively.
References
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Steroid Hormone Metabolites are Barbiturate-Like Modulators of the GABA Receptor
Maria Dorota Majewska,Neil L. Harrison,Rochelle D. Schwartz,Jeffery L. Barker,Steven M. Paul +4 more
TL;DR: Two metabolites of the steroid hormones progesterone and deoxycorticosterone are potent barbiturate-like ligands of the gamma-aminobutyric acid (GABA) receptor-chloride ion channel complex and potentiated the inhibitory actions of GABA in cultured rat hippocampal and spinal cord neurons, which may explain the ability of certain steroid hormones to rapidly alter neuronal excitability.
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Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain.
TL;DR: The presence of allopregnanolone and allotetrahydroDOC in brain is demonstrated and acute stress results in a rapid increase of these neuroactive steroids to levels known to modulate GABAA receptor function.
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Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites.
TL;DR: Two discrete binding sites in the GABAA receptor’s transmembrane domains are identified that mediate the potentiating and direct activation effects of neurosteroids and provide a unique opportunity for the development of new therapeutic, neurosteroid-based ligands and transgenic disease models of Neurosteroid dysfunction.
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Anxiolytic effects of 3α-hydroxy-5α[β]-pregnan-20-one: endogenous metabolites of progesterone that are active at the GABAA receptor
TL;DR: The data suggest that the anxiolytic effect of 3α-hydroxy metabolites of progesterone is mediated by brain GABAA receptors in a stereospecific manner, and are in good agreement with the well-documented in vitro effects of these steroids as potent modulators of the GabAA receptor.
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Anxiolytic activity of the progesterone metabolite 5α-pregnan-3α-ol-20-one
TL;DR: The data indicate that the pregnane steroids produce their anxiolytic effects through a separate mechanism than the BZs, and demonstrate that the endogenous pregnano steroids possess anxioleytic effects that may be clinically relevant.