Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

Metabotropic, but not allosteric, effects of neurosteroids on GABAergic inhibition depend on the phosphorylation of GABAA receptors

(2019) Manasa L. Parakala et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Trial of SAGE-217 in Patients with Major Depressive Disorder

(2019) Handan Gunduz-Bruce et al.   NEW ENGLAND JOURNAL OF MEDICINE

Realising the therapeutic potential of neuroactive steroid modulators of the GABAA receptor

(2019) Delia Belelli et al.   Neurobiology of Stress

GABA A receptor: Positive and negative allosteric modulators

(2018) Richard W. Olsen   NEUROPHARMACOLOGY

An Emerging Circuit Pharmacology of GABA A Receptors

(2018) Elif Engin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Brexanolone injection in post-partum depression: two multicentre, double-blind, randomised, placebo-controlled, phase 3 trials

(2018) Samantha Meltzer-Brody et al.   LANCET

A Novel, Synthetic, Neuroactive Steroid Is Effective at Decreasing Depression-Like Behaviors and Improving Maternal Care in Preclinical Models of Postpartum Depression

(2018) Laverne Melón et al.   Frontiers in Endocrinology

The synthetic neuroactive steroid SGE-516 reduces status epilepticus and neuronal cell death in a rat model of soman intoxication

(2017) Alison L. Althaus et al.   EPILEPSY & BEHAVIOR

Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models

(2017) Rebecca S. Hammond et al.   EPILEPSY RESEARCH

Neurobiological bases of autism-epilepsy comorbidity: a focus on excitation/inhibition imbalance

(2017) Yuri Bozzi et al.   EUROPEAN JOURNAL OF NEUROSCIENCE

Open-label, proof-of-concept study of brexanolone in the treatment of severe postpartum depression

(2017) Stephen J. Kanes et al.   HUMAN PSYCHOPHARMACOLOGY-CLINICAL AND EXPERIMENTAL

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 Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor

(2017) Gabriel Martinez Botella et al.   JOURNAL OF MEDICINAL CHEMISTRY

Brexanolone (SAGE-547 injection) in post-partum depression: a randomised controlled trial

(2017) Stephen Kanes et al.   LANCET

Crystal structures of a GABAA-receptor chimera reveal new endogenous neurosteroid-binding sites

(2017) Duncan Laverty et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

(2017) Amit Modgil et al.   NEUROPHARMACOLOGY

Crystal structures of a GABAA-receptor chimera reveal new endogenous neurosteroid-binding sites

(2017) Duncan Laverty et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The synthetic neuroactive steroid SGE-516 reduces seizure burden and improves survival in a Dravet syndrome mouse model

(2017) Nicole A. Hawkins et al.   Scientific Reports

Parkinson's Disease and Neurodegeneration: GABA-Collapse Hypothesis

(2016) Janusz W. Błaszczyk   Frontiers in Neuroscience

GABA Receptors: Pharmacological Potential and Pitfalls

(2015) Maja Jembrek et al.   CURRENT PHARMACEUTICAL DESIGN

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

(2015) Gabriel Martinez Botella et al.   JOURNAL OF MEDICINAL CHEMISTRY

EEG-β/γ spectral power elevation in rat: a translatable biomarker elicited by GABAAα2/3-positive allosteric modulators at nonsedating anxiolytic doses

(2015) Edward P. Christian et al.   JOURNAL OF NEUROPHYSIOLOGY

The GABAA Receptor as a Therapeutic Target for Neurodevelopmental Disorders

(2015) Sien Braat et al.   NEURON

Neurosteroids promote phosphorylation and membrane insertion of extrasynaptic GABAA receptors

(2014) A. M. Abramian et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Neurosteroid interactions with synaptic and extrasynaptic GABAA receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability

(2013) Chase Matthew Carver et al.   PSYCHOPHARMACOLOGY

Neurosteroids as Therapeutic Leads in Psychiatry

(2013) Charles F. Zorumski et al.   JAMA Psychiatry

Structure, Function, and Modulation of GABAAReceptors

(2012) Erwin Sigel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Benzodiazepines Modulate GABAA Receptors by Regulating the Preactivation Step after GABA Binding

(2012) M. C. Gielen et al.   JOURNAL OF NEUROSCIENCE

Benzodiazepine treatment induces subtype-specific changes in GABAA receptor trafficking and decreases synaptic inhibition

(2012) T. C. Jacob et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Role of GABAAreceptors in the physiology and pharmacology of sleep

(2009) Raphaëlle Winsky-Sommerer   EUROPEAN JOURNAL OF NEUROSCIENCE

Extrasynaptic GABAA Receptors: Form, Pharmacology, and Function

(2009) D. Belelli et al.   JOURNAL OF NEUROSCIENCE

Spastic Hypertonia and Movement Disorders: Pathophysiology, Clinical Presentation, and Quantification

(2009) Geoffrey Sheean et al.   PM&R

Conserved site for neurosteroid modulation of GABAA receptors

(2008) Alastair M. Hosie et al.   NEUROPHARMACOLOGY

GABAA receptors: Subtypes provide diversity of function and pharmacology

(2008) Richard W. Olsen et al.   NEUROPHARMACOLOGY

An automated system for intracellular and intranuclear injection

(2007) Ron C. Hogg et al.   JOURNAL OF NEUROSCIENCE METHODS