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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: rash ks. 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: rash ks. 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 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: rash ks. J Med Chem. 2011 Dec 8;54(23):8000-12. doi: 10.1021/jm200789r. Epub 2011 Oct 26. J Med Chem. 2011. PMID: 21958337
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: rash ks. 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.
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: rash ks. 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.
In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268).
Fell MJ, Perry KW, Falcone JF, Johnson BG, Barth VN, Rash KS, Lucaites VL, Threlkeld PG, Monn JA, McKinzie DL, Marek GJ, Svensson KA, Nelson DL. Fell MJ, et al. Among authors: rash ks. J Pharmacol Exp Ther. 2009 Dec;331(3):1126-36. doi: 10.1124/jpet.109.160598. Epub 2009 Sep 15. J Pharmacol Exp Ther. 2009. PMID: 19755662
18 results