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

Journal of Medicinal Chemistry

Volumn 60, Issue 18, 2017, Pages 7810-7819

  Martinez Botella, Gabriel ^a,d   Salituro, Francesco G ^a   Harrison, Boyd L ^a   Beresis, Richard T ^b   Bai, Zhu ^c   Blanco, Maria Jesus ^a   Belfort, Gabriel M ^a,e   Dai, Jing ^a   Loya, Carlos M ^a,f   Ackley, Michael A ^a   Althaus, Alison L ^a   Grossman, Scott J ^a   Hoffmann, Ethan ^a   Doherty, James J ^a   Robichaud, Albert J ^a  

^a Sage Therapeutics Inc   (United States)

^b Shanghai ChemPartner Co Ltd   (China)

^c WUXI APPTEC   (China)

^d Praxis Precision Medicines   (United States)

^e TAKEDA PHARMACEUTICALS   (United States)

^f Department of Clinical Development Neuroscience Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3ALPHA HYDROXY 3BETA METHYL 21 (4 CYANO 1H PYRAZOL 1' YL) 19 NOR 5BETA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID A RECEPTOR; NEUROSTEROID; PREGNANE DERIVATIVE; SAGE 217; UNCLASSIFIED DRUG; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; ELTANOLONE; PREGNANE-20-ONE; PYRAZOLE DERIVATIVE;

ARTICLE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; NONHUMAN; PHARMACOKINETIC PARAMETERS; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; ALLOSTERISM; ANALOGS AND DERIVATIVES; ANIMAL; CHEMISTRY; DEPRESSION, POSTPARTUM; DEPRESSIVE DISORDER, MAJOR; DRUG EFFECTS; FEMALE; METABOLISM; MOUSE; RAT;

ALLOSTERIC REGULATION; ANIMALS; DEPRESSION, POSTPARTUM; DEPRESSIVE DISORDER, MAJOR; FEMALE; GABA-A RECEPTOR AGONISTS; MICE; PREGNANOLONE; PYRAZOLES; RATS; RECEPTORS, GABA-A;

EID: 85030215849     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b00846     Document Type: Article

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