Search Results - "Johnson, Bryan G"

Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial by Martenyi, Ferenc, Monn, James A, Patil, Sandeep T, Zhang, Lu, Lowe, Stephen L, Jackson, Kimberley A, Andreev, Boris V, Avedisova, Alla S, Bardenstein, Leonid M, Gurovich, Issak Y, Morozova, Margarita A, Mosolov, Sergey N, Neznanov, Nikolai G, Reznik, Alexander M, Smulevich, Anatoly B, Tochilov, Vladimir A, Johnson, Bryan G, Schoepp, Darryle D

“…Schizophrenia is a chronic, complex and heterogeneous mental disorder, with pathological features of disrupted neuronal excitability and plasticity within…”
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Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039) by Fell, Matthew J, Svensson, Kjell A, Johnson, Bryan G, Schoepp, Darryle D

“…(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039) is a potent and selective group II metabotropic glutamate [(mGlu)2…”
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CNS distribution of metabotropic glutamate 2 and 3 receptors: Transgenic mice and [3H]LY459477 autoradiography by Wright, Rebecca A., Johnson, Bryan G., Zhang, Ce, Salhoff, Craig, Kingston, Ann E., Calligaro, David O., Monn, James A., Schoepp, Darryle D., Marek, Gerard J.

“…Group II metabotropic glutamate (mGlu) receptor agonists were efficacious in randomized clinical research trials for schizophrenia and generalized anxiety…”
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Synthesis and Pharmacological Characterization of C4‑(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)‑2-Amino-4-(1H‑1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist by Monn, James A, Prieto, Lourdes, Taboada, Lorena, Hao, Junliang, Reinhard, Matthew R, Henry, Steven S, Beadle, Christopher D, Walton, Lesley, Man, Teresa, Rudyk, Helene, Clark, Barry, Tupper, David, Baker, S. Richard, Lamas, Carlos, Montero, Carlos, Marcos, Alicia, Blanco, Jaime, Bures, Mark, Clawson, David K, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xushan, Carter, Joan H, Getman, Brian G, Catlow, John T, Swanson, Steven, Johnson, Bryan G, Shaw, David B, McKinzie, David L

“…Identification of orthosteric mGlu2/3 receptor agonists capable of discriminating between individual mGlu2 and mGlu3 subtypes has been highly challenging owing…”
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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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Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039) by Rorick-Kehn, Linda M, Johnson, Bryan G, Burkey, Jennifer L, Wright, Rebecca A, Calligaro, David O, Marek, Gerard J, Nisenbaum, Eric S, Catlow, John T, Kingston, Ann E, Giera, Deborah D, Herin, Marc F, Monn, James A, McKinzie, David L, Schoepp, Darryle D

“…Group II metabotropic glutamate (mGlu) receptor agonists, including (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate monohydrate (LY354740) and…”
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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) by Fell, Matthew J, Perry, Kenneth W, Falcone, Julie F, Johnson, Bryan G, Barth, Vanessa N, Rash, Karen S, Lucaites, Virginia L, Threlkeld, Penny G, Monn, James A, McKinzie, David L, Marek, Gerard J, Svensson, Kjell A, Nelson, David L

“…Some recently published in vitro studies with two metabotropic glutamate 2/3 receptor (mGluR(2/3)) agonists [(-)-2-oxa-4-aminobicyclo[3.1.0]…”
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Activation of metabotropic glutamate (mGlu)2 receptors suppresses histamine release in limbic brain regions following acute ketamine challenge by Fell, Matthew J., Katner, Jason S., Johnson, Bryan G., Khilevich, Albert, Schkeryantz, Jeffrey M., Perry, Kenneth W., Svensson, Kjell A.

“…In the present study we demonstrated that ketamine, an NMDA antagonist and possible psychotomimetic, increases extracellular histamine (HA) in the rat brain…”
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Improved bioavailability of the mGlu2/3 receptor agonist LY354740 using a prodrug strategy: in vivo pharmacology of LY544344 by Rorick-Kehn, Linda M, Perkins, Everett J, Knitowski, Karen M, Hart, John C, Johnson, Bryan G, Schoepp, Darryle D, McKinzie, David L

“…Numerous studies have indicated that selective agonists of group II metabotropic glutamate (mGlu) receptors, such as LY354740…”
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Microspine-rubber composite for high friction on smooth, rough, and wet surfaces by Berdan, Constance C., Johnson, Bryan G., Hawkes, Elliot W.

“…As robotic technologies advance and robots move out of factories and labs into the real world, grip on a variety of surfaces (e.g. smooth or rough) in a…”
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Synthesis and Pharmacological Characterization of C4 β -Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu 3 Receptor Agonist by Monn, James A, Henry, Steven S, Massey, Steven M, Clawson, David K, Chen, Qi, Diseroad, Benjamin A, Bhardwaj, Rajni M, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xu-Shan, Carter, Joan H, Getman, Brian G, Adragni, Kofi, Broad, Lisa M, Sanger, Helene E, Ursu, Daniel, Catlow, John T, Swanson, Steven, Johnson, Bryan G, Shaw, David B, McKinzie, David L, Hao, Junliang

“…Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu ) receptors, but small…”
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[ 3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells by Johnson, Bryan G, Wright, Rebecca A, Arnold, M.Brian, Wheeler, William J, Ornstein, Paul L, Schoepp, Darryle D

“…Metabotropic glutamate (mGlu) receptors are a family of eight known subtypes termed mGlu1-8. Currently, few ligands are available to study the pharmacology of…”
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Metabotropic glutamate receptors in the control of mood disorders by Witkin, Jeffrey M, Marek, Gerard J, Johnson, Bryan G, Schoepp, Darryle D

“…Current treatments for depression are less than optimal in terms of onset of action, response and remission rates, and side-effect profiles. Glutamate is the…”
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Synthesis and Structure–Activity Relationship Studies of Novel 2-Diarylethyl Substituted (2-Carboxycycloprop-1-yl)glycines as High-Affinity Group II Metabotropic Glutamate Receptor Ligands by Sørensen, Ulrik S, Bleisch, Thomas J, Kingston, Anne E, Wright, Rebecca A, Johnson, Bryan G, Schoepp, Darryle D, Ornstein, Paul L

“…The major excitatory neurotransmitter in the central nervous system, ( S)-glutamic acid ( 1 ), activates both ionotropic and metabotropic excitatory amino acid…”
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Synthesis and Pharmacological Characterization of 4‑Substituted-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: Identification of New Potent and Selective Metabotropic Glutamate 2/3 Receptor Agonists by Monn, James A, Valli, Matthew J, Massey, Steven M, Hao, Junliang, Reinhard, Matthew R, Bures, Mark G, Heinz, Beverly A, Wang, Xushan, Carter, Joan H, Getman, Brian G, Stephenson, Gregory A, Herin, Marc, Catlow, John T, Swanson, Steven, Johnson, Bryan G, McKinzie, David L, Henry, Steven S

“…As part of our ongoing interest in identifying novel agonists acting at metabotropic glutamate (mGlu) 2/3 receptors, we have explored the effect of structural…”
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Synthesis and Metabotropic Glutamate Receptor Activity of S-Oxidized Variants of (−)-4-Amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate:  Identification of Potent, Selective, and Orally Bioavailable Agonists for mGlu2/3 Receptors by Monn, James A., Massey, Steven M., Valli, Matthew J., Henry, Steven S., Stephenson, Gregory A., Bures, Mark, Hérin, Marc, Catlow, John, Giera, Deborah, Wright, Rebecca A., Johnson, Bryan G., Andis, Sherri L., Kingston, Ann, Schoepp, Darryle D.

“…(−)-4-Amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate (LY389795, (−)-3) is a highly potent and selective agonist of metabotropic glutamate receptors 2…”
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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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Methyl Substitution of 2-Aminobicyclo[3.1.0]hexane 2,6-Dicarboxylate (LY354740) Determines Functional Activity at Metabotropic Glutamate Receptors:  Identification of a Subtype Selective mGlu2 Receptor Agonist by Dominguez, Carmen, Prieto, Lourdes, Valli, Matthew J, Massey, Steven M, Bures, Mark, Wright, Rebecca A, Johnson, Bryan G, Andis, Sherri L, Kingston, Ann, Schoepp, Darryle D, Monn, James A

“…LY354740 (1) is a highly potent and selective agonist of metabotropic glutamate (mGlu) receptors 2 and 3. In the present study, we have prepared C3- and…”
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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 Orexin-1 Antagonist SB-334867 Blocks Antipsychotic Treatment-Emergent Catalepsy: Implications for the Treatment of Extrapyramidal Symptoms by Rasmussen, Kurt, Hsu, Mei-Ann, Noone, Stephen, Johnson, Bryan G., Thompson, Linda K., Hemrick-Luecke, Susan K.

“…We have previously shown that the orexin-1 antagonist SB-334867 blocks the electrophysiological effects of haloperidol and olanzapine on the activity of A9 and…”
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