SAGE-217, A Novel GABAA Receptor Positive Allosteric Modulator: Clinical Pharmacology and Tolerability in Randomized Phase I Dose-Finding Studies
E Hoffmann, GG Nomikos, I Kaul, S Raines… - Clinical …, 2020 - Springer
Background SAGE-217, a novel γ-aminobutyric acid A (GABA A) receptor positive allosteric
modulator, was evaluated in phase I, double-blind, placebo-controlled, single ascending …
modulator, was evaluated in phase I, double-blind, placebo-controlled, single ascending …
[HTML][HTML] Trial of SAGE-217 in patients with major depressive disorder
H Gunduz-Bruce, C Silber, I Kaul… - … England Journal of …, 2019 - Mass Medical Soc
Background Altered neurotransmission of γ-aminobutyric acid (GABA) has been implicated
in the pathogenesis of depression. Whether SAGE-217, an oral, positive allosteric modulator …
in the pathogenesis of depression. Whether SAGE-217, an oral, positive allosteric modulator …
Subtype-selective GABAA receptor modulation yields a novel pharmacological profile: the design and development of TPA023
JR Atack - Advances in Pharmacology, 2009 - Elsevier
Abstract TPA023 is a GABA A α2/α3 subtype-selective modulator which in preclinical
species has anxiolytic-like activity but does not produce sedative-like properties and is …
species has anxiolytic-like activity but does not produce sedative-like properties and is …
An 8-week, randomized, phase 2, double-blind, sequential parallel-group comparison study of two dose levels of the GABAA positive allosteric modulator PF …
A Simen, M Whitlock, R Qiu, J Miceli… - Journal of Clinical …, 2019 - journals.lww.com
Background Generalized anxiety disorder (GAD) is a common psychiatric disorder, but many
patients experience only partial relief of symptoms with existing therapies. Benzodiazepines …
patients experience only partial relief of symptoms with existing therapies. Benzodiazepines …
NS11821, a partial subtype-selective GABAA agonist, elicits selective effects on the central nervous system in randomized controlled trial with healthy subjects
RGJA Zuiker, X Chen, O Østerberg… - Journal of …, 2016 - journals.sagepub.com
NS11821 is a partial GABAA agonist with relatively dominant α2, 3 and α5 subtype efficacy
but negligible α1 agonism. This first-in-human study was performed in healthy male subjects …
but negligible α1 agonism. This first-in-human study was performed in healthy male subjects …
SGS742: the first GABAB receptor antagonist in clinical trials
W Froestl, M Gallagher, H Jenkins, A Madrid… - Biochemical …, 2004 - Elsevier
The GABAB receptor antagonist SGS742 (CGP36742) displays pronounced cognition
enhancing effects in mice, young and old rats and in Rhesus monkeys in active and passive …
enhancing effects in mice, young and old rats and in Rhesus monkeys in active and passive …
NS11394 [3′-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in …
NR Mirza, JS Larsen, C Mathiasen, TA Jacobsen… - … of Pharmacology and …, 2008 - ASPET
The novel positive allosteric modulator NS11394 [3′-[5-(1-hydroxy-1-methyl-ethyl)-
benzoimidazol-1-yl]-biphenyl-2-carbonitrile] possesses a functional selectivity profile at …
benzoimidazol-1-yl]-biphenyl-2-carbonitrile] possesses a functional selectivity profile at …
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABAB receptors
S Guery, P Floersheim, K Kaupmann… - Bioorganic & Medicinal …, 2007 - Elsevier
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of
GABAB receptors - ScienceDirect Skip to main contentSkip to article Elsevier logo Journals & …
GABAB receptors - ScienceDirect Skip to main contentSkip to article Elsevier logo Journals & …
[HTML][HTML] Number needed to treat and number needed to harm analysis of the zuranolone phase 2 clinical trial results in major depressive disorder
A Arnaud, E Suthoff, K Stenson, B Werneburg… - Journal of Affective …, 2021 - Elsevier
Abstract Background Zuranolone (SAGE-217) is a novel, investigational positive allosteric
modulator of GABA A receptors being investigated in major depressive disorder (MDD). This …
modulator of GABA A receptors being investigated in major depressive disorder (MDD). This …
GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors
Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …