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In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist.
Witkin JM, Ornstein PL, Mitch CH, Li R, Smith SC, Heinz BA, Wang XS, Xiang C, Carter JH, Anderson WH, Li X, Broad LM, Pasqui F, Fitzjohn SM, Sanger HE, Smith JL, Catlow J, Swanson S, Monn JA. Witkin JM, et al. Among authors: li x, li r. Neuropharmacology. 2017 Mar 15;115:100-114. doi: 10.1016/j.neuropharm.2015.12.021. Epub 2015 Dec 31. Neuropharmacology. 2017. PMID: 26748052
LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders.
Rorick-Kehn LM, Witkin JM, Statnick MA, Eberle EL, McKinzie JH, Kahl SD, Forster BM, Wong CJ, Li X, Crile RS, Shaw DB, Sahr AE, Adams BL, Quimby SJ, Diaz N, Jimenez A, Pedregal C, Mitch CH, Knopp KL, Anderson WH, Cramer JW, McKinzie DL. Rorick-Kehn LM, et al. Among authors: li x. Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23. Neuropharmacology. 2014. PMID: 24071566
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: li x, li r. 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
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: li x, li r. 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
N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.
Fell MJ, Witkin JM, Falcone JF, Katner JS, Perry KW, Hart J, Rorick-Kehn L, Overshiner CD, Rasmussen K, Chaney SF, Benvenga MJ, Li X, Marlow DL, Thompson LK, Luecke SK, Wafford KA, Seidel WF, Edgar DM, Quets AT, Felder CC, Wang X, Heinz BA, Nikolayev A, Kuo MS, Mayhugh D, Khilevich A, Zhang D, Ebert PJ, Eckstein JA, Ackermann BL, Swanson SP, Catlow JT, Dean RA, Jackson K, Tauscher-Wisniewski S, Marek GJ, Schkeryantz JM, Svensson KA. Fell MJ, et al. Among authors: li x. J Pharmacol Exp Ther. 2011 Jan;336(1):165-77. doi: 10.1124/jpet.110.172957. Epub 2010 Oct 14. J Pharmacol Exp Ther. 2011. PMID: 20947638
Metabotropic Glutamate Receptors Modulate Exocytotic Tau Release and Propagation.
Mazzo F, Butnaru I, Grubisha O, Ficulle E, Sanger H, Fitzgerald G, Pan F, Pasqui F, Murray T, Monn J, Li X, Hutton M, Bose S, Schiavo G, Sher E. Mazzo F, et al. Among authors: li x. J Pharmacol Exp Ther. 2022 Nov;383(2):117-128. doi: 10.1124/jpet.122.001307. Epub 2022 Sep 18. J Pharmacol Exp Ther. 2022. PMID: 36116796
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