D D Schoepp

Summary

Affiliation: Eli Lilly and Company
Country: USA

Publications

  1. ncbi Preclinical pharmacology of mGlu2/3 receptor agonists: novel agents for schizophrenia?
    Darryle D Schoepp DD
    Neuroscience Research Division, Eli Lilly and Company, Indianapolis, Indiana, USA
    Curr Drug Targets CNS Neurol Disord 1:215-25. 2002
  2. ncbi Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system
    D D Schoepp
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Pharmacol Exp Ther 299:12-20. 2001
  3. ncbi 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
    J A Monn
    Core Technology Division, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 39:2990-3000. 1996
  4. ncbi LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors
    D D Schoepp
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropharmacology 36:1-11. 1997
  5. ncbi Anxiolytic-like activity of the mGLU2/3 receptor agonist LY354740 in the elevated plus maze test is disrupted in metabotropic glutamate receptor 2 and 3 knock-out mice
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Psychopharmacology (Berl) 179:284-91. 2005
  6. ncbi 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
    P L Ornstein
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 41:358-78. 1998
  7. ncbi Comparison of c-Fos induction in the brain by the mGlu2/3 receptor antagonist LY341495 and agonist LY354740: evidence for widespread endogenous tone at brain mGlu2/3 receptors in vivo
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropharmacology 49:120-34. 2005
  8. ncbi 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 pr
    J A Monn
    Central Nervous System Division, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 40:528-37. 1997
  9. ncbi Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution
    P L Ornstein
    Lilly Research Laboratories, Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA Ornstein
    J Med Chem 39:2219-31. 1996
  10. ncbi Increased c-Fos expression in the centromedial nucleus of the thalamus in metabotropic glutamate 8 receptor knockout mice following the elevated plus maze test
    A M Linden
    Neuroscience Research Division, Eli Lilly and Company, Lilly Corporate Center, Drop Code 0510, Indianapolis, IN 46285, USA
    Neuroscience 121:167-78. 2003

Collaborators

Detail Information

Publications25

  1. ncbi Preclinical pharmacology of mGlu2/3 receptor agonists: novel agents for schizophrenia?
    Darryle D Schoepp DD
    Neuroscience Research Division, Eli Lilly and Company, Indianapolis, Indiana, USA
    Curr Drug Targets CNS Neurol Disord 1:215-25. 2002
    ....
  2. ncbi Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system
    D D Schoepp
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Pharmacol Exp Ther 299:12-20. 2001
    ..Recent progress on the molecular and pharmacological aspects of these presynaptic mGlu receptors is unveiling their functions and the therapeutic directions of agents designed for these novel glutamate receptor targets...
  3. ncbi 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
    J A Monn
    Core Technology Division, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 39:2990-3000. 1996
    ..It is concluded that (2R,4R)-APDC (2a) is a highly selective, systemically-active agonist of mGluRs negatively coupled to adenylate cyclase and that selective activation of these receptors in vivo can result in anticonvulsant effects...
  4. ncbi LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors
    D D Schoepp
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropharmacology 36:1-11. 1997
    ..Thus, LY354740 is a highly potent, efficacious and selective group II (mGlu2/3) receptor agonist, useful to explore the functions of these receptors in situ...
  5. ncbi Anxiolytic-like activity of the mGLU2/3 receptor agonist LY354740 in the elevated plus maze test is disrupted in metabotropic glutamate receptor 2 and 3 knock-out mice
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Psychopharmacology (Berl) 179:284-91. 2005
    ..However, the lack of mGlu2 or mGlu3 receptor specific agonists has prevented in vivo characterization of individual functions of these two receptors in mediating the anxiolytic-like effects of LY354740...
  6. ncbi 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
    P L Ornstein
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 41:358-78. 1998
    ..p., 60 min preinjection). Thus, 168 represents a valuable tool to study the role of group II mGluRs in disease...
  7. ncbi Comparison of c-Fos induction in the brain by the mGlu2/3 receptor antagonist LY341495 and agonist LY354740: evidence for widespread endogenous tone at brain mGlu2/3 receptors in vivo
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropharmacology 49:120-34. 2005
    ....
  8. ncbi 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 pr
    J A Monn
    Central Nervous System Division, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Med Chem 40:528-37. 1997
    ..6 mg/kg). Thus, (+)-9 is the first orally active group 2 mGluR agonist described thus far and is an important tool for studying the effects of compounds of this class in humans...
  9. ncbi Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution
    P L Ornstein
    Lilly Research Laboratories, Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA Ornstein
    J Med Chem 39:2219-31. 1996
    ....
  10. ncbi Increased c-Fos expression in the centromedial nucleus of the thalamus in metabotropic glutamate 8 receptor knockout mice following the elevated plus maze test
    A M Linden
    Neuroscience Research Division, Eli Lilly and Company, Lilly Corporate Center, Drop Code 0510, Indianapolis, IN 46285, USA
    Neuroscience 121:167-78. 2003
    ..In particular, the deletion of the mGlu8 receptor reduced the threshold of neuronal activation in stress-related brain regions such as the centromedial nucleus of the thalamus...
  11. ncbi 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution
    P L Ornstein
    Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    J Med Chem 41:346-57. 1998
    ..Amino acid 113, with an IC50 of 0.010 microM in the [3H]Glu binding assay, was 52-fold more potent than 2, whose IC50 was 0.47 microM...
  12. ncbi Group III human metabotropic glutamate receptors 4, 7 and 8: molecular cloning, functional expression, and comparison of pharmacological properties in RGT cells
    S Wu
    Research Technology and Protein Division, Drop Code 0424, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Brain Res Mol Brain Res 53:88-97. 1998
    ..The expression and second messenger coupling of human group III mGluRs expressed in the RGT cell line are useful to clearly define the subtype selectivities of mGluR ligands...
  13. ncbi Anxiolytic activity of the MGLU2/3 receptor agonist LY354740 on the elevated plus maze is associated with the suppression of stress-induced c-Fos in the hippocampus and increases in c-Fos induction in several other stress-sensitive brain regions
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropsychopharmacology 29:502-13. 2004
    ....
  14. ncbi Pharmacological agents acting at subtypes of metabotropic glutamate receptors
    D D Schoepp
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Neuropharmacology 38:1431-76. 1999
    ..This article reviews the evolution of pharmacological agents that have been reported to target mGlu receptors, with a focus on the known receptor subtype selectivities of current agents...
  15. ncbi [3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain
    R A Wright
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    J Pharmacol Exp Ther 298:453-60. 2001
    ..These studies indicate that [3H]LY341495 selectively labels group II (mGlu2/3) receptors, but under the conditions used, [3H]LY341495 may bind predominately to mGlu3 receptor populations in the rat forebrain...
  16. ncbi Acute increases in monoamine release in the rat prefrontal cortex by the mGlu2/3 agonist LY379268 are similar in profile to risperidone, not locally mediated, and can be elicited in the presence of uptake blockade
    J Cartmell
    Lilly Research Laboratories, Eli Lilly and Company, IN Indianapolis 46285, USA
    Neuropharmacology 40:847-55. 2001
    ....
  17. ncbi Metabotropic glutamate receptor activation produces extrapyramidal motor system activation that is mediated by striatal dopamine
    A I Sacaan
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285
    J Neurochem 59:245-51. 1992
    ..These results suggest a functional interaction between the metabotropic EAA receptor and the dopaminergic system in the striatum...
  18. ncbi Evaluation of the activity of a novel metabotropic glutamate receptor antagonist (+/-)-2-amino-2-(3-cis and trans-carboxycyclobutyl-3-(9-thioxanthyl)propionic acid) in the in vitro neonatal spinal cord and in an in vivo pain model
    Y Chen
    Eli Lilly and Co, Windlesham, Surrey, UK
    Neuroscience 95:787-93. 2000
    ....
  19. ncbi Neuroprotective actions of novel and potent ligands of group I and group II metabotropic glutamate receptors
    A E Kingston
    Eli Lilly and Co Ltd, Windlesham, Surrey, United Kingdom
    Ann N Y Acad Sci 890:438-49. 1999
    ..These results support the view that antagonists of mGlu1 and mGlu5 and agonists of group II mGlu receptors may be useful agents in the therapeutic treatment of neurodegenerative disease...
  20. ncbi Neuroprotection by metabotropic glutamate receptor glutamate receptor agonists: LY354740, LY379268 and LY389795
    A E Kingston
    Eli Lilly, Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey, UK
    Eur J Pharmacol 377:155-65. 1999
    ..These results suggest that group II mGlu receptor agonists may represent a novel therapeutic strategy for the treatment of neurodegenerative diseases...
  21. ncbi Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles
    D Bleakman
    Eli Lilly and Co, Lilly Research Centre, Windlesham, Surrey, U K
    Neuropharmacology 35:1689-702. 1996
    ..In summary, these results indicate that 2,3-benzodiazepines are potent, selective and stereospecific antagonists of the AMPA subtype of the non-NMDA glutamate receptor...
  22. ncbi Increased anxiety-related behavior in mice deficient for metabotropic glutamate 8 (mGlu8) receptor
    A M Linden
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Neuropharmacology 43:251-9. 2002
    ..Moreover, no significant differences in seizure susceptibility were detected between strains. Our results suggest that mGlu8 receptor may play a role in responses to novel stressful environment...
  23. ncbi Thyrotropin-releasing hormone (protirelin) inhibits potassium-stimulated glutamate and aspartate release from hippocampal slices in vitro
    Y Nie
    Department of Anatomy and Cell Biology, MS 5035, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Brain Res 1054:45-54. 2005
    ..Additional studies are in progress to fully understand the mechanism of this potent effect of TRH and its implication in various CNS disorders...
  24. ncbi Regulation of neurotransmitter release by metabotropic glutamate receptors
    J Cartmell
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    J Neurochem 75:889-907. 2000
    ..This review addresses the neurochemical evidence for mGlu receptor-mediated regulation of neurotransmitters, such as excitatory and inhibitory amino acids, monoamines, and neuropeptides...
  25. ncbi Cloning and expression of a human metabotropic glutamate receptor 1 alpha: enhanced coupling on co-transfection with a glutamate transporter
    M A Desai
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    Mol Pharmacol 48:648-57. 1995
    ..These studies suggest that co-expression of mGluR1 alpha with a glutamate transporter prevents desensitization of the receptor, thus achieving optimal coupling of the receptor with its effector system...