[ Pobierz całość w formacie PDF ]
.ChemMedChem 2:1763 1773256.Vanejevs M, Jatzke C, Renner S et al (2008) Positive and negative modulation of group Imetabotropic glutamate receptors.J Med Chem 51:634 647257.Wang X, Kolasa T, El Kouhen OF et al (2007) Rapid hit to lead evaluation of pyrazolo[3, 4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.Bioorg MedChem Lett 17:4303 4307258.Wu WL, Burnett DA, Domalski M et al (2007) Discovery of orally efficacious tetracyclicmetabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.J Med Chem 50:5550 5553259.Sekhar YN, Nayana MR, Sivakumari N et al (2008) 3D-QSAR and molecular dockingstudies of 1, 3, 5-triazene-2, 4-diamine derivatives against r-RNA: novel bacterial translationinhibitors.J Mol Graph Model 26:1338 1352260.Ito S, Satoh A, Nagatomi Y et al (2008) Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1antagonist.Bioorg Med Chem 16:9817 9829261.Ito S, Hirata Y, Nagatomi Y et al (2009) Discovery and biological profile of isoindolinonederivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment forpsychotic disorders.Bioorg Med Chem Lett 19:5310 5313262.Satoh A, Nagatomi Y, Hirata Y et al (2009) Discovery and in vitro and in vivo profiles of4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methy lbenzamideas novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.Bioorg Med Chem Lett 19:5464 5468263.Helton DR, Tizzano JP, Monn JA et al (1998) Anxiolytic and side-effect profile ofLY354740: a potent, highly selective, orally active agonist for group II metabotropic gluta-mate receptors.J Pharmacol Exp Ther 284:651 660264.Tizzano JP, Griffey KI, Schoepp DD (2002) The anxiolytic action of mGlu2/3 receptoragonist, LY354740, in the fear-potentiated startle model in rats is mechanistically distinctfrom diazepam.Pharmacol Biochem Behav 73:367 374265.Monn JA, Valli MJ, Massey SM et al (1999) Synthesis, pharmacological characterization,and molecular modeling of heterobicyclic amino acids related to ()-2-aminobicyclo[3.1.0]hexane-2, 6-dicarboxylic acid (LY354740): identification of two new potent, selective, andsystemically active agonists for group II metabotropic glutamate receptors.J Med Chem42:1027 1040266.Jones CK, Eberle EL, Peters SC et al (2005) Analgesic effects of the selective group II(mGlu2/3) metabotropic glutamate receptor agonists LY379268 and LY389795 in persis-tent and inflammatory pain models after acute and repeated dosing.Neuropharmacology49(Suppl 1):206 218267.Monn JA, Massey SM, Valli MJ et al (2007) Synthesis and metabotropic glutamate receptoractivity of S-oxidized variants of ( )-4-amino-2-thiabicyclo-[3.1.0]hexane-4, 6-dicarboxy-late: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 recep-tors.J Med Chem 50:233 240268.Rorick-Kehn LM, Johnson BG, Burkey JL et al (2007) Pharmacological and pharmacokineticproperties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptoragonist: in vitro characterization of agonist (-)-(1R, 4S, 5S, 6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4, 6-dicarboxylic acid (LY404039).J Pharmacol Exp Ther 321:308 317 142 E.Schaeffer and A.Duplantier269.Krystal JH, Abi-Saab W, Perry E et al (2005) Preliminary evidence of attenuation of thedisruptive effects of the NMDA glutamate receptor antagonist, ketamine, on workingmemory by pretreatment with the group II metabotropic glutamate receptor agonist,LY354740, in healthy human subjects.Psychopharmacology 179:303 309270.Perkins EJ, Abraham T (2007) Pharmacokinetics, metabolism, and excretion of theintestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S, 2S, 5R, 6S)-2-[(20S)-(2-amino)propionyl]aminobicyclo[3.1.]hexen-2, 6-di carboxylic acid (LY544344) in ratsand dogs: assessment of first-pass bioactivation and dose linearity.Drug Metab Dispos35:1903 1909271.Patil ST, Zhang L, Martenyi F et al (2007) Activation of mGlu2/3 receptors as a newapproach to treat schizophrenia: a randomized Phase 2 clinical trial.Nat Med 13:1102 1107272.Nakazato A, Kumagai T, Sakagami K et al (2000) Synthesis, SARs, and pharmacologicalcharacterization of 2-amino-3 or 6-fluorobicyclo[3.1 [ Pobierz całość w formacie PDF ]
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.ChemMedChem 2:1763 1773256.Vanejevs M, Jatzke C, Renner S et al (2008) Positive and negative modulation of group Imetabotropic glutamate receptors.J Med Chem 51:634 647257.Wang X, Kolasa T, El Kouhen OF et al (2007) Rapid hit to lead evaluation of pyrazolo[3, 4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.Bioorg MedChem Lett 17:4303 4307258.Wu WL, Burnett DA, Domalski M et al (2007) Discovery of orally efficacious tetracyclicmetabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.J Med Chem 50:5550 5553259.Sekhar YN, Nayana MR, Sivakumari N et al (2008) 3D-QSAR and molecular dockingstudies of 1, 3, 5-triazene-2, 4-diamine derivatives against r-RNA: novel bacterial translationinhibitors.J Mol Graph Model 26:1338 1352260.Ito S, Satoh A, Nagatomi Y et al (2008) Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1antagonist.Bioorg Med Chem 16:9817 9829261.Ito S, Hirata Y, Nagatomi Y et al (2009) Discovery and biological profile of isoindolinonederivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment forpsychotic disorders.Bioorg Med Chem Lett 19:5310 5313262.Satoh A, Nagatomi Y, Hirata Y et al (2009) Discovery and in vitro and in vivo profiles of4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methy lbenzamideas novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.Bioorg Med Chem Lett 19:5464 5468263.Helton DR, Tizzano JP, Monn JA et al (1998) Anxiolytic and side-effect profile ofLY354740: a potent, highly selective, orally active agonist for group II metabotropic gluta-mate receptors.J Pharmacol Exp Ther 284:651 660264.Tizzano JP, Griffey KI, Schoepp DD (2002) The anxiolytic action of mGlu2/3 receptoragonist, LY354740, in the fear-potentiated startle model in rats is mechanistically distinctfrom diazepam.Pharmacol Biochem Behav 73:367 374265.Monn JA, Valli MJ, Massey SM et al (1999) Synthesis, pharmacological characterization,and molecular modeling of heterobicyclic amino acids related to ()-2-aminobicyclo[3.1.0]hexane-2, 6-dicarboxylic acid (LY354740): identification of two new potent, selective, andsystemically active agonists for group II metabotropic glutamate receptors.J Med Chem42:1027 1040266.Jones CK, Eberle EL, Peters SC et al (2005) Analgesic effects of the selective group II(mGlu2/3) metabotropic glutamate receptor agonists LY379268 and LY389795 in persis-tent and inflammatory pain models after acute and repeated dosing.Neuropharmacology49(Suppl 1):206 218267.Monn JA, Massey SM, Valli MJ et al (2007) Synthesis and metabotropic glutamate receptoractivity of S-oxidized variants of ( )-4-amino-2-thiabicyclo-[3.1.0]hexane-4, 6-dicarboxy-late: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 recep-tors.J Med Chem 50:233 240268.Rorick-Kehn LM, Johnson BG, Burkey JL et al (2007) Pharmacological and pharmacokineticproperties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptoragonist: in vitro characterization of agonist (-)-(1R, 4S, 5S, 6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4, 6-dicarboxylic acid (LY404039).J Pharmacol Exp Ther 321:308 317 142 E.Schaeffer and A.Duplantier269.Krystal JH, Abi-Saab W, Perry E et al (2005) Preliminary evidence of attenuation of thedisruptive effects of the NMDA glutamate receptor antagonist, ketamine, on workingmemory by pretreatment with the group II metabotropic glutamate receptor agonist,LY354740, in healthy human subjects.Psychopharmacology 179:303 309270.Perkins EJ, Abraham T (2007) Pharmacokinetics, metabolism, and excretion of theintestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S, 2S, 5R, 6S)-2-[(20S)-(2-amino)propionyl]aminobicyclo[3.1.]hexen-2, 6-di carboxylic acid (LY544344) in ratsand dogs: assessment of first-pass bioactivation and dose linearity.Drug Metab Dispos35:1903 1909271.Patil ST, Zhang L, Martenyi F et al (2007) Activation of mGlu2/3 receptors as a newapproach to treat schizophrenia: a randomized Phase 2 clinical trial.Nat Med 13:1102 1107272.Nakazato A, Kumagai T, Sakagami K et al (2000) Synthesis, SARs, and pharmacologicalcharacterization of 2-amino-3 or 6-fluorobicyclo[3.1 [ Pobierz całość w formacie PDF ]