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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: kahl sd. Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23. Neuropharmacology. 2014. PMID: 24071566
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.
Mitch CH, Quimby SJ, Diaz N, Pedregal C, de la Torre MG, Jimenez A, Shi Q, Canada EJ, Kahl SD, Statnick MA, McKinzie DL, Benesh DR, Rash KS, Barth VN. Mitch CH, et al. Among authors: kahl sd. J Med Chem. 2011 Dec 8;54(23):8000-12. doi: 10.1021/jm200789r. Epub 2011 Oct 26. J Med Chem. 2011. PMID: 21958337
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: kahl sd. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Pedregal C, Joshi EM, Toledo MA, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Navarro A, Chen Z, Mudra DR, Kahl SD, Rash KS, Statnick MA, Barth VN. Pedregal C, et al. Among authors: kahl sd. J Med Chem. 2012 Jun 14;55(11):4955-67. doi: 10.1021/jm201629q. Epub 2012 May 16. J Med Chem. 2012. PMID: 22541041
Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.
Hamdouchi C, Maiti P, Warshawsky AM, DeBaillie AC, Otto KA, Wilbur KL, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Cr S, Lineswala JP, Neathery GL, Bouaichi C, Diseroad BA, Campbell AN, Sweetana SA, Adams LA, Cabrera O, Ma X, Yumibe NP, Montrose-Rafizadeh C, Chen Y, Miller AR. Hamdouchi C, et al. Among authors: kahl sd. J Med Chem. 2018 Feb 8;61(3):934-945. doi: 10.1021/acs.jmedchem.7b01411. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29236497
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
Richardson TI, Ornstein PL, Briner K, Fisher MJ, Backer RT, Biggers CK, Clay MP, Emmerson PJ, Hertel LW, Hsiung HM, Husain S, Kahl SD, Lee JA, Lindstrom TD, Martinelli MJ, Mayer JP, Mullaney JT, O'Brien TP, Pawlak JM, Revell KD, Shah J, Zgombick JM, Herr RJ, Melekhov A, Sampson PB, King CH. Richardson TI, et al. Among authors: kahl sd. J Med Chem. 2004 Jan 29;47(3):744-55. doi: 10.1021/jm0304109. J Med Chem. 2004. PMID: 14736255
Potent and selective MC-4 receptor agonists based on a novel disulfide scaffold.
Yan LZ, Flora D, Edwards P, Smiley DL, Emmerson PJ, Hsiung HM, Gadski R, Hertel J, Heiman ML, Husain S, O'Brien TP, Kahl SD, Zhang L, Dimarchi RD, Mayer JP. Yan LZ, et al. Among authors: kahl sd. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4611-4. doi: 10.1016/j.bmcl.2005.06.081. Bioorg Med Chem Lett. 2005. PMID: 16105738
Discovery of a beta-MSH-derived MC-4R selective agonist.
Mayer JP, Hsiung HM, Flora DB, Edwards P, Smith DP, Zhang XY, Gadski RA, Heiman ML, Hertel JL, Emmerson PJ, Husain S, O'brien TP, Kahl SD, Smiley DL, Zhang L, Dimarchi RD, Yan LZ. Mayer JP, et al. Among authors: kahl sd. J Med Chem. 2005 May 5;48(9):3095-8. doi: 10.1021/jm0501432. J Med Chem. 2005. PMID: 15857110
93 results