C C Felder
Affiliation: Eli Lilly and Company
- Cannabinoid receptors and their endogenous agonistsC C Felder
Neuroscience Discovery, ELI LILLY RESEARCH LABORATORY, Indianapolis, Indiana 46285, USA
Annu Rev Pharmacol Toxicol 38:179-200. 1998....
- Scintillation proximity assaySteven D Kahl
Lilly Research Laboratories, Indianapolis, Indiana, USA
Curr Protoc Neurosci . 2005..This unit identifies potential uses of the technology for the measurement of receptor-ligand binding, cAMP accumulation, GTP binding to heterotrimeric G proteins, protease activity and cellular uptake...
- Strategic Research Institute G-Protein-Coupled Receptors Drug Discovery World SummitChristian C Felder
Eli Lilly Research Laboratories, Neuroscience Division, Indianapolis, IN, USA
Expert Opin Investig Drugs 13:1071-4. 2004..GPCRs continue to be an attractive platform for drug discovery...
- 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...
- 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...
- 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...
- 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...
- Determination of [35S]guanosine-5'-O-(3-thio)triphosphate binding mediated by cholinergic muscarinic receptors in membranes from Chinese hamster ovary cells and rat striatum using an anti-G protein scintillation proximity assayN W Delapp
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
J Pharmacol Exp Ther 289:946-55. 1999..Antibody capture GTPgamma35S binding using scintillation proximity assay technology provides a convenient, productive alternative to immunoprecipitation for exploration of receptor-G protein interaction in cells and tissues...
- 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...
- The endocannabinoid nervous system: unique opportunities for therapeutic interventionA C Porter
Neuroscience Division, Drop 0510, Lilly Research Laboratories, Indianapolis, IN 46285, USA
Pharmacol Ther 90:45-60. 2001..This new knowledge may facilitate the development of cannabinoid receptor-targeted therapeutics with improved safety and efficacy profiles...
- N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link betwMatthew J Fell
Neuroscience Discovery Research, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, DC0510, Indianapolis, IN 46285, USA
J Pharmacol Exp Ther 336:165-77. 2011..In addition, we provide evidence that sleep EEG and CSF t-MeHA might function as viable biomarker approaches to facilitate the translational development of THIIC and other mGlu2 potentiators...
- Muscarinic mechanisms of antipsychotic atypicalityFrank P Bymaster
Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
Prog Neuropsychopharmacol Biol Psychiatry 27:1125-43. 2003..However, olanzapine significantly occupies central muscarinic receptors in humans. Overall, the role of muscarinic receptors in the antipsychotic effects of clozapine and olanzapine is controversial and complex...
- Role of specific muscarinic receptor subtypes in cholinergic parasympathomimetic responses, in vivo phosphoinositide hydrolysis, and pilocarpine-induced seizure activityFrank P Bymaster
Neuroscience Research Division, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, USA
Eur J Neurosci 17:1403-10. 2003..Muscarinic M1 receptors appear to be the only muscarinic receptor subtype mediating seizures...
- Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic systemFrank P Bymaster
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
Neurochem Res 28:437-42. 2003..M4 mAChRs modulate dopamine activity in motor tracts and act as inhibitory autoreceptors in striatum. Thus, as elucidated by gene targeting technology, mAChRs have widespread and manifold functions in the periphery and brain...
- M1 muscarinic receptor signaling in mouse hippocampus and cortexAmy C Porter
Lilly Research Laboratories, Neuroscience Research Division, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
Brain Res 944:82-9. 2002..These findings support a role for the M1 receptor subtype as the primary G(alpha)(q)/11-coupled muscarinic receptor in mouse hippocampus and cortex...
- 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...
- 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...
- 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....
- Identification of a high-affinity binding site involved in the transport of endocannabinoidsS A Moore
Eli Lilly and Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285 0510, USA
Proc Natl Acad Sci U S A 102:17852-7. 2005....
- Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitorsAmy K Dickason-Chesterfield
Eli Lilly and Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
Cell Mol Neurobiol 26:407-23. 2006....
- Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophreniaAnantha Shekhar
Department of Psychiatry, Indiana University School of Medicine, 1111 West 10th St, Suite 313, Indianapolis, IN 46202, USA
Am J Psychiatry 165:1033-9. 2008..The authors studied xanomeline, a relatively selective muscarinic type 1 and type 4 (M(1) and M(4)) receptor agonist, to determine if this agent is effective in the treatment of schizophrenia...
- Characterization of a novel endocannabinoid, virodhamine, with antagonist activity at the CB1 receptorAmy C Porter
Lilly Research Laboratories, Neuroscience Division, Eli Lilly and Co, Lilly Corporate Center, Indianapolis, IN, USA
J Pharmacol Exp Ther 301:1020-4. 2002..As a potential endogenous antagonist at the CB1 receptor, virodhamine adds a new form of regulation to the endocannabinoid system...
- Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonistMarla L Watt
Lilly Research Laboratories, Eli Lilly and Co, Lilly Corporate Center, Indianapolis, IN 46285, USA
J Pharmacol Exp Ther 338:622-32. 2011..This compound demonstrates modest to no activity at the other muscarinic receptor subtypes, stimulates Gα(q)-coupled signaling events as well as β-arrestin recruitment, and displays significant efficacy in in vivo models of cognition...
- Evaluation of muscarinic agonist-induced analgesia in muscarinic acetylcholine receptor knockout miceAlokesh Duttaroy
Laboratory of Bioorganic Chemistry, National Institute of Diabetes Digestive and Kidney Diseases, Bethesda, Maryland 20892 0810, USA
Mol Pharmacol 62:1084-93. 2002..These findings should be of considerable relevance for the development of receptor subtype-selective muscarinic agonists as novel analgesic drugs...
- New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug)Vindhya Nawaratne
Drug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Clayton, Victoria 3800, Australia
Mol Pharmacol 74:1119-31. 2008..These results provide conclusive evidence for the retention of a functional allosteric site on the M4 DREADD and highlight a role for residues Tyr113 and Ala203 in the transmission of cooperativity...
- Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brainArieh Moussaieff
Department of Medicinal Chemistry and Natural Products, Medical Faculty, Hebrew University of Jerusalem, 91120, Jerusalem, Israel
FASEB J 22:3024-34. 2008..Furthermore, the biochemical and pharmacological effects of IA may provide a biological basis for deeply rooted cultural and religious traditions...
- Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodentsGarth Terry
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
Neuroimage 41:690-8. 2008..Radiometabolites of [11C]MePPEP in brain caused distribution volume to be overestimated by approximately 13%...
- The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brainFumihiko Yasuno
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
Neuropsychopharmacology 33:259-69. 2008..These promising results in monkey justify studying this radioligand in human subjects...
- Muscarinic receptor subtypes mediating central and peripheral antinociception studied with muscarinic receptor knockout mice: a reviewJurgen Wess
Laboratory of Bioorganic Chemistry, Molecular Signaling Section, National Institute of Diabetes and Digestive and Kidney Diseases, Bldg 8A, Room B1A 05, 8 Center Drive MSC 0810, Bethesda, MD 20892 0810, USA
Life Sci 72:2047-54. 2003..Our results highlight the usefulness of muscarinic receptor mutant mice to shed light on the functional roles of acetylcholine released from both neuronal and non-neuronal cells...