F P Bymaster

Summary

Affiliation: Eli Lilly and Company
Country: USA

Publications

  1. ncbi request reprint Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Neuropsychopharmacology 25:871-80. 2001
  2. ncbi request reprint Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects
    F P Bymaster
    Lilly Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Brain Res 795:179-90. 1998
  3. ncbi request reprint Elucidating the role of muscarinic receptors in psychosis
    C C Felder
    Neuroscience Division, Eli Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Life Sci 68:2605-13. 2001
  4. ncbi request reprint Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity
    P Sauerberg
    Health Care Discovery, Novo Nordisk A S, Novo Nordisk Park, 2760 Malov, Denmark, and Neuroscience Research, Lilly Research Laboratories, Indianapolis, Indiana 46285, USA
    J Med Chem 41:4378-84. 1998
  5. ncbi request reprint Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats
    H E Shannon
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    J Pharmacol Exp Ther 290:901-7. 1999
  6. ncbi request reprint Investigations into the physiological role of muscarinic M2 and M4 muscarinic and M4 receptor subtypes using receptor knockout mice
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285 0510, USA
    Life Sci 68:2473-9. 2001
  7. ncbi request reprint The muscarinic M1 agonist xanomeline increases soluble amyloid precursor protein release from Chinese hamster ovary-m1 cells
    K Eckols
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    Life Sci 57:1183-90. 1995
  8. ncbi request reprint Dysregulated hippocampal acetylcholine neurotransmission and impaired cognition in M2, M4 and M2/M4 muscarinic receptor knockout mice
    E T Tzavara
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Psychiatry 8:673-9. 2003
  9. ncbi request reprint Arachidonic acid release in cell lines transfected with muscarinic receptors: a simple functional assay to determine response of agonists
    F P Bymaster
    Lilly Neuroscience Research, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Cell Signal 11:405-13. 1999
  10. ncbi request reprint Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Schizophr Res 37:107-22. 1999

Collaborators

Detail Information

Publications33

  1. ncbi request reprint Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Neuropsychopharmacology 25:871-80. 2001
    ..9 and 94 mg/kg for blocking p-chloramphetamine- and 6-hydroxydopamine-induced monoamine depletion, respectively. Thus, duloxetine more potently blocks 5-HT and NE transporters in vitro and in vivo than venlafaxine...
  2. ncbi request reprint Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects
    F P Bymaster
    Lilly Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Brain Res 795:179-90. 1998
    ....
  3. ncbi request reprint Elucidating the role of muscarinic receptors in psychosis
    C C Felder
    Neuroscience Division, Eli Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Life Sci 68:2605-13. 2001
    ..These findings support a role for the development of M1 and M4 receptor agonists for diseases in which symptoms include cognitive impairment and psychotic behaviors...
  4. ncbi request reprint Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity
    P Sauerberg
    Health Care Discovery, Novo Nordisk A S, Novo Nordisk Park, 2760 Malov, Denmark, and Neuroscience Research, Lilly Research Laboratories, Indianapolis, Indiana 46285, USA
    J Med Chem 41:4378-84. 1998
    ..A model explaining the potency differences of closely related compounds is offered. The data suggest that muscarinic agonists act as functional dopamine antagonists and that they could become a novel treatment of psychotic patients...
  5. ncbi request reprint Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats
    H E Shannon
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    J Pharmacol Exp Ther 290:901-7. 1999
    ....
  6. ncbi request reprint Investigations into the physiological role of muscarinic M2 and M4 muscarinic and M4 receptor subtypes using receptor knockout mice
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285 0510, USA
    Life Sci 68:2473-9. 2001
    ..The data demonstrate the usefulness of knockout mice in determining the physiological function of peripheral and central muscarinic receptors...
  7. ncbi request reprint The muscarinic M1 agonist xanomeline increases soluble amyloid precursor protein release from Chinese hamster ovary-m1 cells
    K Eckols
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
    Life Sci 57:1183-90. 1995
    ..These results demonstrate that xanomeline increased APPs release by activation of m1 muscarinic receptors and support the possibility that cholinergic replacement therapy for Alzheimer's Disease may reduce amyloid deposition...
  8. ncbi request reprint Dysregulated hippocampal acetylcholine neurotransmission and impaired cognition in M2, M4 and M2/M4 muscarinic receptor knockout mice
    E T Tzavara
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Mol Psychiatry 8:673-9. 2003
    ..Together these results suggest a crucial role for muscarinic M2 and M4 receptors in the tonic and phasic regulation of acetylcholine efflux in the hippocampus as well as in cognitive processes...
  9. ncbi request reprint Arachidonic acid release in cell lines transfected with muscarinic receptors: a simple functional assay to determine response of agonists
    F P Bymaster
    Lilly Neuroscience Research, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Cell Signal 11:405-13. 1999
    ..It is concluded that arachidonic acid release is a simple assay suitable for evaluation of muscarinic agonists, antagonists and the flux of external calcium into cells...
  10. ncbi request reprint Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Schizophr Res 37:107-22. 1999
    ..Olanzapine was a weaker antagonist at muscarinic and dopamine D1 receptors...
  11. ncbi request reprint Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice
    H E Shannon
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Schizophr Res 42:249-59. 2000
    ....
  12. ncbi request reprint Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Eur J Pharmacol 390:245-8. 2000
    ..5 to 73 nM in intact cells. These data suggest that the affinity of olanzapine and clozapine for muscarinic receptors have been significantly overestimated...
  13. ncbi request reprint Receptor reserve of phosphoinositide-coupled muscarinic receptors in mouse hippocampus in vivo
    F P Bymaster
    Neuroscience Research Division, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
    Brain Res 916:165-71. 2001
    ..Since pilocarpine is a relatively weak partial agonist, these data suggest a substantial level of receptor reserve for the PI response in mouse hippocampus...
  14. ncbi request reprint The cannabinoid CB(1) receptor antagonist SR141716A increases norepinephrine outflow in the rat anterior hypothalamus
    E T Tzavara
    Eli Lilly and Company, Lilly Corporate Center, Neuroscience Discovery Research, Indianapolis, IN 46285-0510, USA
    Eur J Pharmacol 426:R3-4. 2001
    ..This increase in norepinephrine outflow could play an important role in the pharmacological and potentially therapeutic actions of SR141716A...
  15. ncbi request reprint 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...
  16. ncbi request reprint The muscarinic agonist xanomeline increases monoamine release and immediate early gene expression in the rat prefrontal cortex
    K W Perry
    Eli Lilly and Company Research Laboratories, Neuroscience Research Division, Lilly Corporate Center, Indianapolis, IN 46285-0510, USA
    Biol Psychiatry 49:716-25. 2001
    ..Based on the antipsychotic-like activity of xanomeline in Alzheimer's patients and the similarity to atypical antipsychotic agents, we suggest that xanomeline may be a novel antipsychotic agent...
  17. ncbi request reprint Olanzapine vs haloperidol in geriatric schizophrenia: analysis of data from a double-blind controlled trial
    J S Kennedy
    Indiana University School of Medicine, Department of Psychiatry, Indianapolis, Indiana, USA
    Int J Geriatr Psychiatry 18:1013-20. 2003
    ..To compare the six-week clinical response and safety profile of schizophrenia patients, age > or =60 years, receiving olanzapine (OLZ) vs haloperidol (HAL) in a double blind, randomized trial...
  18. ncbi request reprint Role of the cholinergic muscarinic system in bipolar disorder and related mechanism of action of antipsychotic agents
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Indianapolis, IN 46285 0510, USA
    Mol Psychiatry 7:S57-63. 2002
    ..Olanzapine may normalize mood due to antidepressant-like activities, such as 5-HT(2A) receptor antagonism and increasing cortical norepinephrine and dopamine...
  19. ncbi request reprint Muscarinic agonist-mediated increases in serum corticosterone levels are abolished in m(2) muscarinic acetylcholine receptor knockout mice
    S K Hemrick-Luecke
    Neuroscience Division, Lilly Research Laboratories, Eli Lilly and Co, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    J Pharmacol Exp Ther 303:99-103. 2002
    ..These data suggest that the muscarinic M(2) receptor subtype mediates muscarinic agonist-induced activation of the hypothalamic-pituitary-adrenocortical axis in mice...
  20. ncbi request reprint Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine
    F P Bymaster
    Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0501, USA
    Eur J Pharmacol 430:341-9. 2001
    ..Thus, olanzapine was not an agonist, but was a potent antagonist at 5-HT(6) receptors and had marked antagonism at 5-HT(3) receptors...
  21. pmc Minocycline prevents nigrostriatal dopaminergic neurodegeneration in the MPTP model of Parkinson's disease
    Y Du
    Departmens of Pharmacology and Toxicology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Proc Natl Acad Sci U S A 98:14669-74. 2001
    ..Thus, NO appears to play an important role in MPTP neurotoxicity. Neuroprotective tetracyclines may be effective in preventing or slowing the progression of Parkinson's and other neurodegenerative diseases...
  22. ncbi request reprint Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake
    F P Bymaster
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Bioorg Med Chem Lett 13:4477-80. 2003
    ..One member of this series, duloxetine (Cymbalta) has proven to be effective in clinical trials for the treatment of depression...
  23. ncbi request reprint A current review of olanzapine's safety in the geriatric patient: from pre-clinical pharmacology to clinical data
    J S Kennedy
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    Int J Geriatr Psychiatry 16:S33-61. 2001
    ....
  24. ncbi request reprint Procholinergic and memory enhancing properties of the selective norepinephrine uptake inhibitor atomoxetine
    E T Tzavara
    Eli Lilly and Company, Lilly Corporate Center, Neuroscience Discovery Research, Indianapolis, IN 46285, USA
    Mol Psychiatry 11:187-95. 2006
    ..We showed that, consistent with its cortical procholinergic and catecholamine-enhancing profile, atomoxetine (1-3 mg/kg, p.o.) significantly ameliorated performance in the object recognition test and the radial arm-maze test...
  25. ncbi request reprint Current perspectives on the development of non-biogenic amine-based antidepressants
    P Skolnick
    Neuroscience Discovery, Eli Lilly and Co, Lilly Corporate Center, DC 0510, Indianapolis, IN 46285 0510, USA
    Pharmacol Res 43:411-23. 2001
    ..Drugs emerging from these strategies may offer significant advantages over currently used antidepressants...
  26. ncbi request reprint Muscarinic receptors in schizophrenia
    B Dean
    The Rebecca L Cooper Research Laboratories, The Mental Health Research Institute of Victoria, Parkville, Victoria, Australia
    Curr Mol Med 3:419-26. 2003
    ..This review presents data from diverse areas of research to argue that it is now imperative that the therapeutic potential of manipulating the activity of muscarinic receptors for the treatment of schizophrenia is fully explored...
  27. pmc Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout mice
    M Yamada
    Laboratory of Bioorganic Chemistry National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 98:14096-101. 2001
    ....
  28. ncbi request reprint Generation and pharmacological analysis of M2 and M4 muscarinic receptor knockout mice
    J Gomeza
    Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD 20892, USA
    Life Sci 68:2457-66. 2001
    ..These findings emphasize the usefulness of gene targeting approaches to shed light on the physiological and pathophysiological roles of the individual muscarinic receptor subtypes...
  29. ncbi request reprint The procholinergic effects of the atypical antipsychotic olanzapine are independent of muscarinic autoreceptor inhibition
    E T Tzavara
    Mol Psychiatry 11:619-21. 2006
  30. ncbi request reprint M1-M5 muscarinic receptor knockout mice as novel tools to study the physiological roles of the muscarinic cholinergic system
    J Wess
    Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 20892, USA
    Receptors Channels 9:279-90. 2003
    ..These results should offer new perspectives for the rational development of novel muscarinic drugs...
  31. ncbi request reprint The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidance
    T Rasmussen
    Health Care Discovery, Novo Nordisk A/S, Novo Nordisk Park, DK-2760, , Denmark
    Schizophr Res 49:193-201. 2001
    ..3), sertindole (3) and olanzapine (3). These data suggest that BuTAC is a potential novel antipsychotic which may have favourable effects on aspects of learning and memory...
  32. ncbi request reprint Towards a muscarinic hypothesis of schizophrenia
    T J Raedler
    Department of Psychiatry, University Medical Center Hamburg Eppendorf, Hamburg, Germany
    Mol Psychiatry 12:232-46. 2007
    ....
  33. pmc Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia
    W Y Chan
    Neuroscience Discovery Research, Lilly Research Centre, Surrey GU20 6PH, United Kingdom
    Proc Natl Acad Sci U S A 105:10978-83. 2008
    ..Importantly, LY2033298 was active in animal models predictive of clinical antipsychotic drug efficacy indicating its potential use as a first-in-class, selective, allosteric muscarinic antipsychotic agent...