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Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.
Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH. Dressman BA, et al. Among authors: blanco mj. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. doi: 10.1016/j.bmcl.2016.10.067. Epub 2016 Oct 25. Bioorg Med Chem Lett. 2016. PMID: 27836401
Target engagement in lead generation.
Durham TB, Blanco MJ. Durham TB, et al. Among authors: blanco mj. Bioorg Med Chem Lett. 2015 Mar 1;25(5):998-1008. doi: 10.1016/j.bmcl.2014.12.076. Epub 2015 Jan 12. Bioorg Med Chem Lett. 2015. PMID: 25630223 Free article. Review.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores.
Zhang D, Blanco MJ, Ying BP, Kohlman D, Liang SX, Victor F, Chen Q, Krushinski J, Filla SA, Hudziak KJ, Mathes BM, Cohen MP, Zacherl D, Nelson DL, Wainscott DB, Nutter SE, Gough WH, Schaus JM, Xu YC. Zhang D, et al. Among authors: blanco mj. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4337-41. doi: 10.1016/j.bmcl.2015.07.042. Epub 2015 Jul 22. Bioorg Med Chem Lett. 2015. PMID: 26271587
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.
Blanco MJ, Benesh DR, Knobelsdorf JA, Khilevich A, Cortez GS, Mokube F, Aicher TD, Groendyke TM, Marmsater FP, Tang TP, Johnson KW, Clemens-Smith A, Muhlhauser MA, Swanson S, Catlow J, Emkey R, Johnson MP, Schkeryantz JM. Blanco MJ, et al. Bioorg Med Chem Lett. 2017 Jan 15;27(2):323-328. doi: 10.1016/j.bmcl.2016.11.049. Epub 2016 Nov 18. Bioorg Med Chem Lett. 2017. PMID: 27908761
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL. Chappell MD, et al. Among authors: blanco mj. J Med Chem. 2016 Dec 22;59(24):10974-10993. doi: 10.1021/acs.jmedchem.6b01119. Epub 2016 Dec 6. J Med Chem. 2016. PMID: 28002967
Analgesic and anti-inflammatory properties of novel, selective, and potent EP4 receptor antagonists.
Chandrasekhar S, Yu XP, Harvey AK, Oskins JL, Lin C, Wang X, Blanco MJ, Fisher MJ, Kuklish SL, Schiffler MA, Vetman T, Warshawsky AM, York JS, Bendele AM, Chambers MG. Chandrasekhar S, et al. Among authors: blanco mj. Pharmacol Res Perspect. 2017 May 14;5(3):e00316. doi: 10.1002/prp2.316. eCollection 2017 Jun. Pharmacol Res Perspect. 2017. PMID: 28603634 Free PMC article.
132 results