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Mapping the neurosteroid binding sites on glycine receptors
(Pergamon-Elsevier Science Ltd, 2019-09)
Glycine is a major inhibitory neurotransmitter in the CNS, where it modulates both sensory and motor transduction throughout its binding to glycine receptors (GlyRs), pentameric chloride channels that share structural and ...
Structure and dynamics of neurosteroid binding to the α1β2γ2 GABAA receptor
(Pergamon-Elsevier Science Ltd, 2018-09-01)
Neurosteroids are the principal endogenous modulators of the γ-Aminobutyric acid receptors (GABAARs), pentameric membrane-bound proteins that can be assembled from at least 19 subunits. In the most abundant GABAAR arrangement ...
Exploring the molecular basis of neurosteroid binding to the β3 homopentameric GABAA receptor
(Elsevier, 2015-11)
Neurosteroids are the principal endogenous modulators of GABAA receptors (GABAARs), which are pentameric membrane-bound proteins that regulate the passage of chloride ions from the extracellular to the intracellular ...
Neurosteroids and neuropathic pain: an up-to-date perspective
(Elsevier, 2022-02)
This perspective aims to broaden our view on the role of neurosteroids, especially progesterone, allopregnanolone, and dehydroepiandrosterone, in the regulation of neuropathic pain. We will make special emphasis on new ...
In Search of GABAA Receptor's Neurosteroid Binding Sites
(American Chemical Society, 2019-06)
Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors (GABAARs), which are the ligand-gated channels target of the major inhibitory neurotransmitter in vertebrates. As a consequence of their ...
Synthesis of 6-thia analogs of the natural neurosteroid allopregnanolone
(Elsevier, 2006)
A procedure is described for the preparation of 6-thiapregnanes in five steps from pregnenolone via a 5-oxo-7-iodo-secopregnane intermediate. The 6-thiasteroid obtained was converted into 6-thia-allopregnanolone and its ...
Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs
(Elsevier, 2008-01)
Three analogs of neuroactive steroids were prepared (4–6) in which 1,11- or 11,19-oxygen bridges give a constrained conformation. Their 3D structures were obtained by ab initio calculations and in the case of 3α-hydroxy- ...
Synthetic neurosteroids on brain protection
(Neural Regeneration Research, 2015-02-17)
Neurosteroids, like allopregnanolone and pregnanolone, are endogenous regulators of neuronal excitability. Inside the brain, they are highly selective and potent modulators of GABAA receptor activity. Their anticonvulsant, ...
Synthesis and GABA(A) receptor activity of oxygen-bridged neurosteroid analogs
(2008)
Three analogs of neuroactive steroids were prepared (4-6) in which 1,11- or 11,19-oxygen bridges give a constrained conformation. Their 3D structures were obtained by ab initio calculations and in the case of 3 ...
Injury elicited increase in spinal cord neurosteroid content analysed by gas chromatography mass espectrometry
(Endocrine Society, 2006-04)
The effects of spinal cord injury (SCI), combined with castration and adrenalectomy, and of progesterone (PROG) treatment on neurosteroid levels and steroidogenic enzyme expression were investigated in the adult male rat ...