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(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: tizzano jp. J Med Chem. 2004 Jan 15;47(2):456-66. doi: 10.1021/jm030967o. J Med Chem. 2004. PMID: 14711315
Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s).
Johnson MP, Barda D, Britton TC, Emkey R, Hornback WJ, Jagdmann GE, McKinzie DL, Nisenbaum ES, Tizzano JP, Schoepp DD. Johnson MP, et al. Among authors: tizzano jp. Psychopharmacology (Berl). 2005 Apr;179(1):271-83. doi: 10.1007/s00213-004-2099-9. Epub 2005 Feb 17. Psychopharmacology (Berl). 2005. PMID: 15717213
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: tizzano jp. J Med Chem. 2005 Aug 11;48(16):5305-20. doi: 10.1021/jm050235r. J Med Chem. 2005. PMID: 16078848
Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase.
Monn JA, Valli MJ, Johnson BG, Salhoff CR, Wright RA, Howe T, Bond A, Lodge D, Spangle LA, Paschal JW, Campbell JB, Griffey K, Tizzano JP, Schoepp DD. Monn JA, et al. Among authors: tizzano jp. J Med Chem. 1996 Jul 19;39(15):2990-3000. doi: 10.1021/jm9601765. J Med Chem. 1996. PMID: 8709133
Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties.
Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Monn JA, et al. Among authors: tizzano jp. J Med Chem. 1997 Feb 14;40(4):528-37. doi: 10.1021/jm9606756. J Med Chem. 1997. PMID: 9046344
2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.
Ornstein PL, Bleisch TJ, Arnold MB, Kennedy JH, Wright RA, Johnson BG, Tizzano JP, Helton DR, Kallman MJ, Schoepp DD, Hérin M. Ornstein PL, et al. Among authors: tizzano jp. J Med Chem. 1998 Jan 29;41(3):358-78. doi: 10.1021/jm970498o. J Med Chem. 1998. PMID: 9464367
34 results