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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: witkin jm. Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23. Neuropharmacology. 2014. PMID: 24071566
Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders.
Bruns RF, Mitchell SN, Wafford KA, Harper AJ, Shanks EA, Carter G, O'Neill MJ, Murray TK, Eastwood BJ, Schaus JM, Beck JP, Hao J, Witkin JM, Li X, Chernet E, Katner JS, Wang H, Ryder JW, Masquelin ME, Thompson LK, Love PL, Maren DL, Falcone JF, Menezes MM, Zhang L, Yang CR, Svensson KA. Bruns RF, et al. Among authors: witkin jm. Neuropharmacology. 2018 Jan;128:351-365. doi: 10.1016/j.neuropharm.2017.10.032. Epub 2017 Oct 26. Neuropharmacology. 2018. PMID: 29102759
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. Neuropharmacology. 2017 Mar 15;115:100-114. doi: 10.1016/j.neuropharm.2015.12.021. Epub 2015 Dec 31. Neuropharmacology. 2017. PMID: 26748052
Anxiolytic-like effects through a GLUK5 kainate receptor mechanism.
Alt A, Weiss B, Ornstein PL, Gleason SD, Bleakman D, Stratford RE Jr, Witkin JM. Alt A, et al. Among authors: witkin jm. Neuropharmacology. 2007 Jun;52(7):1482-7. doi: 10.1016/j.neuropharm.2007.02.005. Epub 2007 Mar 2. Neuropharmacology. 2007. PMID: 17418283
In vivo occupancy of dopamine D3 receptors by antagonists produces neurochemical and behavioral effects of potential relevance to attention-deficit-hyperactivity disorder.
Barth V, Need AB, Tzavara ET, Giros B, Overshiner C, Gleason SD, Wade M, Johansson AM, Perry K, Nomikos GG, Witkin JM. Barth V, et al. Among authors: witkin jm. J Pharmacol Exp Ther. 2013 Feb;344(2):501-10. doi: 10.1124/jpet.112.198895. Epub 2012 Nov 29. J Pharmacol Exp Ther. 2013. PMID: 23197772
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