Research Topics
Species | F P BymasterSummaryAffiliation: Eli Lilly and Company Country: USA Publications
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Publications
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptorsF 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...- Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effectsF P Bymaster
Lilly Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
Brain Res 795:179-90. 1998.... - Elucidating the role of muscarinic receptors in psychosisC 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... - Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activityP 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... - Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in ratsH E Shannon
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
J Pharmacol Exp Ther 290:901-7. 1999.... - Investigations into the physiological role of muscarinic M2 and M4 muscarinic and M4 receptor subtypes using receptor knockout miceF 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... - The muscarinic M1 agonist xanomeline increases soluble amyloid precursor protein release from Chinese hamster ovary-m1 cellsK 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... - Dysregulated hippocampal acetylcholine neurotransmission and impaired cognition in M2, M4 and M2/M4 muscarinic receptor knockout miceE 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... - Arachidonic acid release in cell lines transfected with muscarinic receptors: a simple functional assay to determine response of agonistsF 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... - Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitroF 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... - Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and miceH E Shannon
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Schizophr Res 42:249-59. 2000.... - Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological mediumF 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... - Receptor reserve of phosphoinositide-coupled muscarinic receptors in mouse hippocampus in vivoF 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... - The cannabinoid CB(1) receptor antagonist SR141716A increases norepinephrine outflow in the rat anterior hypothalamusE 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... - Metabotropic glutamate receptor activation produces extrapyramidal motor system activation that is mediated by striatal dopamineA 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... - The muscarinic agonist xanomeline increases monoamine release and immediate early gene expression in the rat prefrontal cortexK 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... - Olanzapine vs haloperidol in geriatric schizophrenia: analysis of data from a double-blind controlled trialJ 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... - Role of the cholinergic muscarinic system in bipolar disorder and related mechanism of action of antipsychotic agentsF 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... - Muscarinic agonist-mediated increases in serum corticosterone levels are abolished in m(2) muscarinic acetylcholine receptor knockout miceS 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... - Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapineF 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... 
Minocycline prevents nigrostriatal dopaminergic neurodegeneration in the MPTP model of Parkinson's diseaseY 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...- Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptakeF 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... - A current review of olanzapine's safety in the geriatric patient: from pre-clinical pharmacology to clinical dataJ S Kennedy
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
Int J Geriatr Psychiatry 16:S33-61. 2001.... - Procholinergic and memory enhancing properties of the selective norepinephrine uptake inhibitor atomoxetineE 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... - Current perspectives on the development of non-biogenic amine-based antidepressantsP 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... - Muscarinic receptors in schizophreniaB 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... - Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout miceM 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.... - Generation and pharmacological analysis of M2 and M4 muscarinic receptor knockout miceJ 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... - The procholinergic effects of the atypical antipsychotic olanzapine are independent of muscarinic autoreceptor inhibitionE T Tzavara
Mol Psychiatry 11:619-21. 2006 - M1-M5 muscarinic receptor knockout mice as novel tools to study the physiological roles of the muscarinic cholinergic systemJ 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... - The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidanceT 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... - Towards a muscarinic hypothesis of schizophreniaT J Raedler
Department of Psychiatry, University Medical Center Hamburg Eppendorf, Hamburg, Germany
Mol Psychiatry 12:232-46. 2007.... - Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophreniaW 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...