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Synthesis and pharmacological characterization of C4-disubstituted analogs of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: identification of a potent, selective metabotropic glutamate receptor agonist and determination of agonist-bound human mGlu2 and mGlu3 amino terminal domain structures.
Monn JA, Prieto L, Taboada L, Pedregal C, Hao J, Reinhard MR, Henry SS, Goldsmith PJ, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Xiang C, Catlow JT, Swanson S, Sanger H, Broad LM, Johnson MP, Knopp KL, Simmons RM, Johnson BG, Shaw DB, McKinzie DL. Monn JA, et al. Among authors: pedregal c. J Med Chem. 2015 Feb 26;58(4):1776-94. doi: 10.1021/jm501612y. Epub 2015 Feb 5. J Med Chem. 2015. PMID: 25602126
Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
Bueno AB, Collado I, de Dios A, Domínguez C, Martín JA, Martín LM, Martínez-Grau MA, Montero C, Pedregal C, Catlow J, Coffey DS, Clay MP, Dantzig AH, Lindstrom T, Monn JA, Jiang H, Schoepp DD, Stratford RE, Tabas LB, Tizzano JP, Wright RA, Herin MF. Bueno AB, et al. Among authors: pedregal c. J Med Chem. 2005 Aug 11;48(16):5305-20. doi: 10.1021/jm050235r. J Med Chem. 2005. PMID: 16078848
C3'-cis-Substituted carboxycyclopropyl glycines as metabotropic glutamate 2/3 receptor agonists: synthesis and SAR studies.
González R, Collado I, de Uralde BL, Marcos A, Martín-Cabrejas LM, Pedregal C, Blanco-Urgoiti J, Pérez-Castells J, Fernández MA, Andis SL, Johnson BG, Wright RA, Schoepp DD, Monn JA. González R, et al. Among authors: pedregal c. Bioorg Med Chem. 2005 Dec 1;13(23):6556-70. doi: 10.1016/j.bmc.2005.07.036. Epub 2005 Sep 8. Bioorg Med Chem. 2005. PMID: 16153851
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
Collado I, Pedregal C, Bueno AB, Marcos A, González R, Blanco-Urgoiti J, Pérez-Castells J, Schoepp DD, Wright RA, Johnson BG, Kingston AE, Moher ED, Hoard DW, Griffey KI, Tizzano JP. Collado I, et al. Among authors: pedregal c. J Med Chem. 2004 Jan 15;47(2):456-66. doi: 10.1021/jm030967o. J Med Chem. 2004. PMID: 14711315
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: pedregal c. 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: pedregal c. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
26 results