Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive …

G Martinez Botella, FG Salituro… - Journal of Medicinal …, 2017 - ACS Publications
Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of
synaptic and extrasynaptic GABAA receptors. Herein, we report new SAR insights in a series …

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid …

FG Salituro, BL Harrison, RT Beresis, Z Bai… - Journal of Medicinal …, 2017 - europepmc.org
Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of
synaptic and extrasynaptic GABA A receptors. Herein, we report new SAR insights in a …

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure–Activity Relationships of Heterocyclic Substitution at C-21

G Martinez Botella, FG Salituro… - Journal of Medicinal …, 2015 - ACS Publications
Neuroactive steroids (NASs) have been shown to impact central nervous system (CNS)
function through positive allosteric modulation of the GABAA receptor (GABAA-R). Herein …

Structure-activity relationships of neuroactive steroids acting on the GABAA receptor

AS Veleiro, G Burton - Current medicinal chemistry, 2009 - ingentaconnect.com
The term “neuroactive steroid”(NAS) refers to steroids which, independent of their origin, are
capable of modifying neural activities. These steroids positively or negatively modulate the …

Effects on γ-aminobutyric acid (GABA) A receptors of a neuroactive steroid that negatively modulates glutamate neurotransmission and augments GABA …

S Mennerick, CM Zeng, A Benz, W Shen, Y Izumi… - Molecular …, 2001 - ASPET
Neurosteroids positively and negatively modulate γ-aminobutyric acid (GABA) A receptors
and glutamate receptors, which underlie most fast inhibition and excitation in the central …

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

D Covey, AJ Robichaud - US Patent 9,630,986, 2017 - Google Patents
Wu, Pharmaceuticals (2009) 2: 77-81. Jiang. X., et al., Neurosteroid analogues. 9.
Conformationally constrained pregnanes: structure-activity studies of 13.24-cyclo 18, 21 …

Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders

M Gasior, RB Carter, JM Witkin - Trends in pharmacological sciences, 1999 - cell.com
Neuroactive steroids are a novel class of positive allosteric modulators of the GABA A
receptor. Although neuroactive steroids are endogenous neuronal modulators, synthetic …

Endogenous and synthetic neuroactive steroids evoke sustained increases in the efficacy of GABAergic inhibition via a protein kinase C-dependent mechanism

A Modgil, ML Parakala, MA Ackley, JJ Doherty… - …, 2017 - Elsevier
The neuroactive steroid (NAS) tetrahydrodeoxycorticosterone (THDOC) increases protein
kinase C (PKC) mediated phosphorylation of extrasynaptic GABA A receptor (GABA AR) …

Neurosteroids promote phosphorylation and membrane insertion of extrasynaptic GABAA receptors

AM Abramian, E Comenencia-Ortiz… - Proceedings of the …, 2014 - National Acad Sciences
Neurosteroids are synthesized within the brain and act as endogenous anxiolytic,
anticonvulsant, hypnotic, and sedative agents, actions that are principally mediated via their …

Site-specific effects of neurosteroids on GABAA receptor activation and desensitization

Y Sugasawa, WWL Cheng, JR Bracamontes, ZW Chen… - Elife, 2020 - elifesciences.org
This study examines how site-specific binding to three identified neurosteroid-binding sites
in the α1β3 GABAA receptor (GABAAR) contributes to neurosteroid allosteric modulation …