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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: barth vn. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography.
Pike VW, Rash KS, Chen Z, Pedregal C, Statnick MA, Kimura Y, Hong J, Zoghbi SS, Fujita M, Toledo MA, Diaz N, Gackenheimer SL, Tauscher JT, Barth VN, Innis RB. Pike VW, et al. Among authors: barth vn. J Med Chem. 2011 Apr 28;54(8):2687-700. doi: 10.1021/jm101487v. Epub 2011 Mar 25. J Med Chem. 2011. PMID: 21438532 Free PMC article.
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: barth vn. J Med Chem. 2011 Dec 8;54(23):8000-12. doi: 10.1021/jm200789r. Epub 2011 Oct 26. J Med Chem. 2011. PMID: 21958337
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: barth vn. J Med Chem. 2012 Jun 14;55(11):4955-67. doi: 10.1021/jm201629q. Epub 2012 May 16. J Med Chem. 2012. PMID: 22541041
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. Among authors: barth vn. 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.
Brain and whole-body imaging in rhesus monkeys of 11C-NOP-1A, a promising PET radioligand for nociceptin/orphanin FQ peptide receptors.
Kimura Y, Fujita M, Hong J, Lohith TG, Gladding RL, Zoghbi SS, Tauscher JA, Goebl N, Rash KS, Chen Z, Pedregal C, Barth VN, Pike VW, Innis RB. Kimura Y, et al. Among authors: barth vn. J Nucl Med. 2011 Oct;52(10):1638-45. doi: 10.2967/jnumed.111.091181. Epub 2011 Aug 30. J Nucl Med. 2011. PMID: 21880575 Free PMC article.
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Gardinier KM, et al. Among authors: barth vn. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29. J Med Chem. 2016. PMID: 27067148
37 results