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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.
Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Blanco MJ, Belfort GM, Dai J, Loya CM, Ackley MA, Althaus AL, Grossman SJ, Hoffmann E, Doherty JJ, Robichaud AJ. Martinez Botella G, et al. Among authors: belfort gm. J Med Chem. 2017 Sep 28;60(18):7810-7819. doi: 10.1021/acs.jmedchem.7b00846. Epub 2017 Aug 17. J Med Chem. 2017. PMID: 28753313
Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator.
Althaus AL, Ackley MA, Belfort GM, Gee SM, Dai J, Nguyen DP, Kazdoba TM, Modgil A, Davies PA, Moss SJ, Salituro FG, Hoffmann E, Hammond RS, Robichaud AJ, Quirk MC, Doherty JJ. Althaus AL, et al. Among authors: belfort gm. Neuropharmacology. 2020 Dec 15;181:108333. doi: 10.1016/j.neuropharm.2020.108333. Epub 2020 Sep 22. Neuropharmacology. 2020. PMID: 32976892 Free PMC article.
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.
Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Shen K, Belfort GM, Loya CM, Ackley MA, Grossman SJ, Hoffmann E, Jia S, Wang J, Doherty JJ, Robichaud AJ. Martinez Botella G, et al. Among authors: belfort gm. J Med Chem. 2015 Apr 23;58(8):3500-11. doi: 10.1021/acs.jmedchem.5b00032. Epub 2015 Apr 14. J Med Chem. 2015. PMID: 25799373
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