J
Joseph P. Tizzano
Researcher at Eli Lilly and Company
Publications - 44
Citations - 3294
Joseph P. Tizzano is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: Metabotropic glutamate receptor & Agonist. The author has an hindex of 25, co-authored 44 publications receiving 3215 citations.
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Journal ArticleDOI
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.
James A. Monn,Matthew John Valli,Steven March Massey,Rebecca A. Wright,Craig R. Salhoff,Bryan G. Johnson,Trevor J. Howe,Charles A. Alt,Rhodes Gary Anthony,Roger L. Robey,Kelly R. Griffey,Joseph P. Tizzano,Mary Jeanne Kallman,David R. Helton,Darryle D. Schoepp +14 more
TL;DR: In this paper, the authors showed that 9 would closely approximate the bioactive conformation of glutamate when acting at group 2 metabotropic glutamate receptors (mGluRs) in the rat cerebral cortical slice.
Journal ArticleDOI
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.
James A. Monn,Matthew John Valli,Steven Marc Massey,Marvin M. Hansen,Kress Thomas Joseph,James P. Wepsiec,Harkness Allen Robert,John L. Grutsch,Rebecca A. Wright,Bryan G. Johnson,Sherri L. Andis,Ann E. Kingston,Rosemarie Tomlinson,Richard A. Lewis,Kelly R. Griffey,Joseph P. Tizzano,Darryle D. Schoepp +16 more
TL;DR: Evaluation of the functional effects of (-)-9 and (-)-10 on second-messenger responses in nonneuronal cells expressing human mGlu receptor subtypes demonstrated each to be a highly potent agonist for group II mGLU receptors.
Journal Article
Anxiolytic and Side-Effect Profile of LY354740: A Potent, Highly Selective, Orally Active Agonist for Group II Metabotropic Glutamate Receptors
TL;DR: A functional role for group II mGluRs in fear/anxiety responses in animals is indicated and compounds in this class may be beneficial in the treatment of anxiety-related disorders in humans without the side effects seen with currently prescribed medications.
Journal ArticleDOI
Antidepressant-like actions of an AMPA receptor potentiator (LY392098).
TL;DR: Findings indicate that biarylpropylsulfonamides, exemplified by LY392098, may represent a novel class of antidepressants.
Journal ArticleDOI
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.
Michael P. Johnson,Melvyn Baez,G. Erik Jagdmann,Thomas C. Britton,Thomas H. Large,David O. Callagaro,Joseph P. Tizzano,James A. Monn,Darryle D. Schoepp +8 more
TL;DR: Recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors pyridylmethylsulfonamides potentiate glutamate, shifting agonist potency by 2-fold, and represent the first mGLU2 receptor potentiators discovered.