Search Results - "TIZZANO, Joseph P"

In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders by RORICK-KEHN, Linda M, JOHNSON, Bryan G, SCHOEPP, Darryle D, KNITOWSKI, Karen M, SALHOFF, Craig R, WITKIN, Jeffrey M, PERRY, Kenneth W, GRIFFEY, Kelly I, TIZZANO, Joseph P, MONN, James A, MCKINZIE, David L

“…Data from both preclinical and clinical studies have provided proof of concept that modulation of limbic and forebrain glutamate, via mGlu2/3 receptor…”
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Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s) by Johnson, Michael P, Barda, David, Britton, Thomas C, Emkey, Renee, Hornback, William J, Jagdmann, G Erik, McKinzie, David L, Nisenbaum, Eric S, Tizzano, Joseph P, Schoepp, Darryle D

“…To increase subtype selectivity and provide a novel means to alter receptor function, we discovered and characterization potentiators for the metabotropic…”
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Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor:  Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine by Johnson, Michael P, Baez, Melvyn, Jagdmann, G. Erik, Britton, Thomas C, Large, Thomas H, Callagaro, David O, Tizzano, Joseph P, Monn, James A, Schoepp, Darryle D

“…This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3)…”
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Preclinical evaluation of the abuse potential of the analgesic bicifadine by Nicholson, Katherine L, Balster, Robert L, Golembiowska, Krystyna, Kowalska, Magdalena, Tizzano, Joseph P, Skolnick, Phil, Basile, Anthony S

“…The abuse liability of the analgesic bicifadine was investigated in animal models used to predict the abuse potential of psychostimulants in humans…”
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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 by Monn, James A, Valli, Matthew J, Massey, Steven M, Wright, Rebecca A, Salhoff, Craig R, Johnson, Bryan G, Howe, Trevor, Alt, Charles A, Rhodes, Gary A, Robey, Roger L, Griffey, Kelly R, Tizzano, Joseph P, Kallman, Mary J, Helton, David R, Schoepp, Darryle D

“…2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (9) was designed as a conformationally constrained analog of glutamic acid. For 9, the key torsion angles (τ1…”
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The anxiolytic action of mGlu2/3 receptor agonist, LY354740, in the fear-potentiated startle model in rats is mechanistically distinct from diazepam by Tizzano, Joseph P., Griffey, Kelly I., Schoepp, Darryle D.

“…The fear-potentiated startle paradigm has been characterized for drugs that act via ionotropic (NMDA and AMPA/kainate receptor) glutamate receptor mechanisms…”
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The triple uptake inhibitor (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0] hexane hydrochloride (DOV 21947) reduces body weight and plasma triglycerides in rodent models of diet-induced obesity by Tizzano, Joseph P, Stribling, D Sloan, Perez-Tilve, Diego, Strack, Alison, Frassetto, Andrea, Chen, Richard Z, Fong, Tung M, Shearman, Lauren, Krieter, Philip A, Tschöp, Matthias H, Skolnick, Phil, Basile, Anthony S

“…Selective inhibitors of biogenic amine (e.g., serotonin, norepinephrine, and dopamine) uptake exhibit varying degrees of safety and efficacy as antiobesity…”
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Antidepressant-like actions of an AMPA receptor potentiator (LY392098) by Li, Xia, Tizzano, Joseph P, Griffey, Kelly, Clay, Michael, Lindstrom, Terry, Skolnick, Phil

“…LY392098 is a member of a novel class of biarylpropylsulfonamides that potentiates AMPA receptor-mediated responses both in vitro and in vivo. In this study,…”
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Anxiolytic and side-effect profile of LY354740: a potent, highly selective, orally active agonist for group II metabotropic glutamate receptors by Helton, D R, Tizzano, J P, Monn, J A, Schoepp, D D, Kallman, M J

“…LY354740 is a conformationally constrained analog of glutamate which is a potent agonist for group II cAMP coupled metabotropic glutamate receptors (mGluRs)…”
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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, and Systemically Active Agonists for Group II Metabotropic Glutamate Receptors by Monn, James A, Valli, Matthew J, Massey, Steven M, Hansen, Marvin M, Kress, Thomas J, Wepsiec, James P, Harkness, Allen R, Grutsch, John L, Wright, Rebecca A, Johnson, Bryan G, Andis, Sherri L, Kingston, Ann, Tomlinson, Rosemarie, Lewis, Richard, Griffey, Kelly R, Tizzano, Joseph P, Schoepp, Darryle D

“…As part of our ongoing research program aimed at the identification of highly potent, selective, and systemically active agonists for group II metabotropic…”
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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 by Bueno, Ana Belén, Collado, Iván, de Dios, Alfonso, Domínguez, Carmen, Martín, José Alfredo, Martín, Luisa M, Martínez-Grau, María Angeles, Montero, Carlos, Pedregal, Concepción, Catlow, John, Coffey, D. Scott, Clay, Michael P, Dantzig, Anne H, Lindstrom, Terry, Monn, James A, Jiang, Haiyan, Schoepp, Darryle D, Stratford, Robert E, Tabas, Linda B, Tizzano, Joseph P, Wright, Rebecca A, Herin, Marc F

“…(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (1), also known as LY354740, is a highly potent and selective agonist for group II metabotropic glutamate…”
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Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors by Ornstein, Paul L, Zimmerman, Dennis M, Arnold, M. Brian, Bleisch, Thomas J, Cantrell, Buddy, Simon, Richard, Zarrinmayeh, Hamideh, Baker, S. Richard, Gates, Mary, Tizzano, Joseph P, Bleakman, David, Mandelzys, Allan, Jarvie, Kieth R, Ho, Ken, Deverill, Michelle, Kamboj, Rajender K

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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 by Collado, Iván, Pedregal, Concepción, Bueno, Ana Belén, Marcos, Alicia, González, Rosario, Blanco-Urgoiti, Jaime, Pérez-Castells, Javier, Schoepp, Darryle D, Wright, Rebecca A, Johnson, Bryan G, Kingston, Ann E, Moher, Eric D, Hoard, David W, Griffey, Kelly I, Tizzano, Joseph P

“…The asymmetric synthesis and biological activity of (2S,1‘S,2‘R,3‘R)-2-(2‘-carboxy-3‘-hydroxymethylcyclopropyl) glycine ((+)-3) is described. This novel C-3‘…”
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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 by Ornstein, Paul L, Bleisch, Thomas J, Arnold, M. Brian, Kennedy, Joseph H, Wright, Rebecca A, Johnson, Bryan G, Tizzano, Joseph P, Helton, David R, Kallman, Mary Jeanne, Schoepp, Darryle D, Hérin, Marc

“…In this paper we describe the synthesis of a series of α-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR)…”
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Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagonists by Kingston, Ann E, Griffey, Kelly, Johnson, Michael P, Chamberlain, Mary-Jo, Kelly, Gerald, Tomlinson, Rosemarie, Wright, Rebecca A, Johnson, Bryan G, Schoepp, Darryle D, Harris, John R, Clark, Barry P, Baker, Richard S, Tizzano, Joseph P

“…A series of novel group I metabotropic glutamate receptor (mGlu) antagonists have been designed on the basis of the 4-carboxyphenylglycine pharmacophore. The…”
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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 by Monn, James A, Valli, Matthew J, Johnson, Bryan G, Salhoff, Craig R, Wright, Rebecca A, Howe, Trevor, Bond, Ann, Lodge, David, Spangle, Larry A, Paschal, Jonathan W, Campbell, Jack B, Griffey, Kelly, Tizzano, Joseph P, Schoepp, Darryle D

“…The four isomers of 4-aminopyrrolidine-2,4-dicarboxylate (APDC) were prepared and evaluated for their effects at glutamate receptors in vitro. (2R,4R)-APDC…”
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Synthesis of a Series of Aryl Kainic Acid Analogs and Evaluation in Cells Stably Expressing the Kainate Receptor humGluR6 by Cantrell, Buddy E, Zimmerman, Dennis M, Monn, James A, Kamboj, Rajender K, Hoo, Ken H, Tizzano, Joseph P, Pullar, Ian A, Farrell, Louise N, Bleakman, David

“…The synthesis and pharmacological characterization of a novel series of 4-aryl-substituted kainic acid analogs are described. Receptor affinities were…”
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(3SR,4aRS,6SR,8aRS)-6-(1H-Tetrazol-5-yl)decahydroisoquinoline-3-carboxylic Acid, a Novel, Competitive, Systemically Active NMDA and AMPA Receptor Antagonist by Ornstein, Paul L, Arnold, M. Brian, Allen, Nancy K, Leander, J. David, Tizzano, Joseph P, Lodge, David, Schoepp, Darryle D

“…We report the synthesis and characterization of 6 (LY246492), which is a competitive N-methyl-D-aspartate (NMDA) and…”
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Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor : Synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethyl- amine by JOHNSON, Michael P, BAEZ, Melvyn, JAGDMANN, G. Erik, BRITTON, Thomas C, LARGE, Thomas H, CALLAGARO, David O, TIZZANO, Joseph P, MONN, James A, SCHOEPP, Darryle D

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The anxiolytic action of mGlu2/3 receptor agonist, LY354740, in the fear-potentiated startle model in rats is mechanistically distinct from diazepam: Metabotropic glutamate receptors by TIZZANO, Joseph P, GRIFFEY, Kelly I, SCHOEPP, Darryle D

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