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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
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
A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models.
Rorick-Kehn LM, Ciccocioppo R, Wong CJ, Witkin JM, Martinez-Grau MA, Stopponi S, Adams BL, Katner JS, Perry KW, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Weiss F, Statnick MA. Rorick-Kehn LM, et al. Among authors: witkin jm. Alcohol Clin Exp Res. 2016 May;40(5):945-54. doi: 10.1111/acer.13052. Epub 2016 Apr 16. Alcohol Clin Exp Res. 2016. PMID: 27084498 Free PMC article.
In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders.
Rorick-Kehn LM, Johnson BG, Knitowski KM, Salhoff CR, Witkin JM, Perry KW, Griffey KI, Tizzano JP, Monn JA, McKinzie DL, Schoepp DD. Rorick-Kehn LM, et al. Among authors: witkin jm. Psychopharmacology (Berl). 2007 Jul;193(1):121-36. doi: 10.1007/s00213-007-0758-3. Epub 2007 Mar 24. Psychopharmacology (Berl). 2007. PMID: 17384937
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM, Kahl SD, Rash KS, Mudra DR, Barth VN, Shaw DB, McKinzie D, Witkin JM, Statnick MA. Toledo MA, et al. Among authors: witkin jm. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
A Novel Nociceptin Receptor Antagonist LY2940094 Inhibits Excessive Feeding Behavior in Rodents: A Possible Mechanism for the Treatment of Binge Eating Disorder.
Statnick MA, Chen Y, Ansonoff M, Witkin JM, Rorick-Kehn L, Suter TM, Song M, Hu C, Lafuente C, Jiménez A, Benito A, Diaz N, Martínez-Grau MA, Toledo MA, Pintar JE. Statnick MA, et al. Among authors: witkin jm. J Pharmacol Exp Ther. 2016 Feb;356(2):493-502. doi: 10.1124/jpet.115.228221. Epub 2015 Dec 9. J Pharmacol Exp Ther. 2016. PMID: 26659925
Preclinical findings predicting efficacy and side-effect profile of LY2940094, an antagonist of nociceptin receptors.
Witkin JM, Rorick-Kehn LM, Benvenga MJ, Adams BL, Gleason SD, Knitowski KM, Li X, Chaney S, Falcone JF, Smith JW, Foss J, Lloyd K, Catlow JT, McKinzie DL, Svensson KA, Barth VN, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Martínez-Grau MA, Post A, Ansonoff MA, Pintar JE, Statnick MA. Witkin JM, et al. Pharmacol Res Perspect. 2016 Nov 7;4(6):e00275. doi: 10.1002/prp2.275. eCollection 2016 Dec. Pharmacol Res Perspect. 2016. PMID: 28097008 Free PMC article.
249 results