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Page 1
Neuroactive Steroid N-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.
La DS, Salituro FG, Martinez Botella G, Griffin AM, Bai Z, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lewis MC, Quirk MC, Robichaud AJ. La DS, et al. Among authors: harrison bl. J Med Chem. 2019 Aug 22;62(16):7526-7542. doi: 10.1021/acs.jmedchem.9b00591. Epub 2019 Aug 13. J Med Chem. 2019. PMID: 31390523
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: harrison bl. 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
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: harrison bl. 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
Breakthroughs in neuroactive steroid drug discovery.
Blanco MJ, La D, Coughlin Q, Newman CA, Griffin AM, Harrison BL, Salituro FG. Blanco MJ, et al. Among authors: harrison bl. Bioorg Med Chem Lett. 2018 Jan 15;28(2):61-70. doi: 10.1016/j.bmcl.2017.11.043. Epub 2017 Dec 2. Bioorg Med Chem Lett. 2018. PMID: 29223589 Review.
SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
Hill MD, Blanco MJ, Salituro FG, Bai Z, Beckley JT, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lanzetta D, Lewis M, Quirk MC, Robichaud AJ. Hill MD, et al. Among authors: harrison bl. J Med Chem. 2022 Jul 14;65(13):9063-9075. doi: 10.1021/acs.jmedchem.2c00313. Epub 2022 Jul 2. J Med Chem. 2022. PMID: 35785990
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.
Bernotas RC, Antane S, Shenoy R, Le VD, Chen P, Harrison BL, Robichaud AJ, Zhang GM, Smith D, Schechter LE. Bernotas RC, et al. Among authors: harrison bl. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1657-60. doi: 10.1016/j.bmcl.2010.01.073. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138763
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Havran LM, Chong DC, Childers WE, Dollings PJ, Dietrich A, Harrison BL, Marathias V, Tawa G, Aulabaugh A, Cowling R, Kapoor B, Xu W, Mosyak L, Moy F, Hum WT, Wood A, Robichaud AJ. Havran LM, et al. Among authors: harrison bl. Bioorg Med Chem. 2009 Nov 15;17(22):7755-68. doi: 10.1016/j.bmc.2009.09.036. Epub 2009 Sep 24. Bioorg Med Chem. 2009. PMID: 19836248
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.
Bernotas RC, Antane SA, Lenicek SE, Haydar SN, Robichaud AJ, Harrison BL, Zhang GM, Smith D, Coupet J, Schechter LE. Bernotas RC, et al. Among authors: harrison bl. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6935-8. doi: 10.1016/j.bmcl.2009.10.067. Epub 2009 Oct 20. Bioorg Med Chem Lett. 2009. PMID: 19884004
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Ghiron C, Haydar SN, Aschmies S, Bothmann H, Castaldo C, Cocconcelli G, Comery TA, Di L, Dunlop J, Lock T, Kramer A, Kowal D, Jow F, Grauer S, Harrison B, La Rosa S, Maccari L, Marquis KL, Micco I, Nencini A, Quinn J, Robichaud AJ, Roncarati R, Scali C, Terstappen GC, Turlizzi E, Valacchi M, Varrone M, Zanaletti R, Zanelli U. Ghiron C, et al. J Med Chem. 2010 Jun 10;53(11):4379-89. doi: 10.1021/jm901692q. J Med Chem. 2010. PMID: 20465311
79 results