D
David R. Helton
Researcher at Eli Lilly and Company
Publications - 28
Citations - 1477
David R. Helton 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 15, co-authored 28 publications receiving 1464 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 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.
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LY354740: a metabotropic glutamate receptor agonist which ameliorates symptoms of nicotine withdrawal in rats
TL;DR: Data support the functional role of mGluR agonists in nicotine withdrawal and indicate that LY354740 may be efficacious in reducing the symptoms associated with nicotine withdrawal during smoking cessation in humans.
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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
Paul L. Ornstein,Thomas J. Bleisch,Arnold Macklin Brian,Joseph H. Kennedy,Rebecca A. Wright,Bryan G. Johnson,Joseph P. Tizzano,David R. Helton,and Mary Jeanne Kallman,Darryle D. Schoepp,M. Herin +10 more
TL;DR: The synthesis of a series of alpha-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1'S,2'S)-carboxycyclopropylglycine (2, L-CCG 1) and the effects of substitution on the aromatic ring as a strategy to increase the affinity to these compounds for group II mGluRs are explored.
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Nicotine withdrawal: a behavioral assessment using schedule controlled responding, locomotor activity, and sensorimotor reactivity.
TL;DR: These studies indicate that rats display increased sensorimotor reactivity after cessation of chronic nicotine exposure, and 2) the expression of nicotine dependence and withdrawal is dependent on the behavioral task employed.