quinoxalines

Summary

Top Publications

  1. pmc Risk of cardiovascular serious adverse events associated with varenicline use for tobacco cessation: systematic review and meta-analysis
    Judith J Prochaska
    Department of Psychiatry and Center for Tobacco Control Research and Education, University of California, San Francisco, CA 94143 0984, USA
    BMJ 344:e2856. 2012
  2. ncbi Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis
    Montserrat Camps
    Serono Pharmaceutical Research Institute, Serono International S A, 14, Chemin des Aulx, 1228 Plan les Ouates, Geneva, Switzerland
    Nat Med 11:936-43. 2005
  3. pmc Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking
    Pia Steensland
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, 5858 Horton Street, Suite 200, Emeryville, CA 94608, USA
    Proc Natl Acad Sci U S A 104:12518-23. 2007
  4. pmc Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysis
    Sonal Singh
    Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, USA
    CMAJ 183:1359-66. 2011
  5. pmc Efficacy and safety of varenicline for smoking cessation in patients with cardiovascular disease: a randomized trial
    Nancy A Rigotti
    General Medicine Division, Department of Medicine, Massachusetts General Hospital, Harvard Medical School, Tobacco Research and Treatment Center, Boston, Mass 02114, USA
    Circulation 121:221-9. 2010
  6. ncbi BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice
    James R Burke
    Department of Immunology, Inflammation and Pulmonary Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    J Biol Chem 278:1450-6. 2003
  7. pmc Varenicline reduces alcohol self-administration in heavy-drinking smokers
    Sherry A McKee
    Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut 06519, USA
    Biol Psychiatry 66:185-90. 2009
  8. ncbi Alpha2 adrenergic modulation of NMDA receptor function as a major mechanism of RGC protection in experimental glaucoma and retinal excitotoxicity
    Cun Jian Dong
    Department of Biological Sciences, Allergan Pharmaceuticals, Irvine, California 92612, USA
    Invest Ophthalmol Vis Sci 49:4515-22. 2008
  9. ncbi Varenicline for smoking cessation: a placebo-controlled, randomized study
    Chen Wang
    Department of Epidemiology, Beijing Institute of Respiratory Medicine, WHO Collaborating Center for Tobacco or Health, Beijing Chao Yang Hospital Affiliated, Capital Medical University, Beijing, China
    Respirology 14:384-92. 2009
  10. ncbi Modular competition driven by NMDA receptor subtypes in spike-timing-dependent plasticity
    Richard C Gerkin
    Center for Neuroscience, University of Pittsburgh, Pittsburgh, PA, USA
    J Neurophysiol 97:2851-62. 2007

Detail Information

Publications314 found, 100 shown here

  1. pmc Risk of cardiovascular serious adverse events associated with varenicline use for tobacco cessation: systematic review and meta-analysis
    Judith J Prochaska
    Department of Psychiatry and Center for Tobacco Control Research and Education, University of California, San Francisco, CA 94143 0984, USA
    BMJ 344:e2856. 2012
    ..To examine the risk of treatment emergent, cardiovascular serious adverse events associated with varenicline use for tobacco cessation...
  2. ncbi Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis
    Montserrat Camps
    Serono Pharmaceutical Research Institute, Serono International S A, 14, Chemin des Aulx, 1228 Plan les Ouates, Geneva, Switzerland
    Nat Med 11:936-43. 2005
    ..Our results identify selective PI3Kgamma inhibitors as potential therapeutic molecules for the treatment of chronic inflammatory disorders such as rheumatoid arthritis...
  3. pmc Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking
    Pia Steensland
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, 5858 Horton Street, Suite 200, Emeryville, CA 94608, USA
    Proc Natl Acad Sci U S A 104:12518-23. 2007
    ..The selectivity of varenicline in decreasing ethanol consumption combined with its reported safety profile and mild side effects in humans suggest that varenicline may prove to be a treatment for alcohol dependence...
  4. pmc Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysis
    Sonal Singh
    Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, USA
    CMAJ 183:1359-66. 2011
    ..We conducted a systematic review and meta-analysis of randomized controlled trials to ascertain the serious adverse cardiovascular effects of varenicline compared with placebo among tobacco users...
  5. pmc Efficacy and safety of varenicline for smoking cessation in patients with cardiovascular disease: a randomized trial
    Nancy A Rigotti
    General Medicine Division, Department of Medicine, Massachusetts General Hospital, Harvard Medical School, Tobacco Research and Treatment Center, Boston, Mass 02114, USA
    Circulation 121:221-9. 2010
    ..Varenicline, a partial alpha4beta2 nicotinic acetylcholine receptor agonist, is effective for smoking cessation in healthy smokers, but its efficacy and safety in smokers with cardiovascular disease are unknown...
  6. ncbi BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice
    James R Burke
    Department of Immunology, Inflammation and Pulmonary Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    J Biol Chem 278:1450-6. 2003
    ..Thus, the compound is effective against NF-kappa B activation in mice and represents an important tool for investigating the role of IKK in disease models...
  7. pmc Varenicline reduces alcohol self-administration in heavy-drinking smokers
    Sherry A McKee
    Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut 06519, USA
    Biol Psychiatry 66:185-90. 2009
    ..Varenicline, a partial nicotinic agonist with high affinity for the alpha4beta2 nAChR receptor, reduced ethanol intake in rodents. We aimed to test whether varenicline would reduce alcohol consumption and alcohol craving in humans...
  8. ncbi Alpha2 adrenergic modulation of NMDA receptor function as a major mechanism of RGC protection in experimental glaucoma and retinal excitotoxicity
    Cun Jian Dong
    Department of Biological Sciences, Allergan Pharmaceuticals, Irvine, California 92612, USA
    Invest Ophthalmol Vis Sci 49:4515-22. 2008
    ..In this study, the authors investigated the neural mechanism that may underlie alpha2 neuroprotection of RGCs...
  9. ncbi Varenicline for smoking cessation: a placebo-controlled, randomized study
    Chen Wang
    Department of Epidemiology, Beijing Institute of Respiratory Medicine, WHO Collaborating Center for Tobacco or Health, Beijing Chao Yang Hospital Affiliated, Capital Medical University, Beijing, China
    Respirology 14:384-92. 2009
    ..This study evaluated the efficacy of a standard regimen of varenicline compared with placebo for smoking cessation in 333 subjects in China, Singapore and Thailand...
  10. ncbi Modular competition driven by NMDA receptor subtypes in spike-timing-dependent plasticity
    Richard C Gerkin
    Center for Neuroscience, University of Pittsburgh, Pittsburgh, PA, USA
    J Neurophysiol 97:2851-62. 2007
    ..Using a simple model, we show that such a modular competition recapitulates our observations...
  11. pmc Activin-like kinase 5 (ALK5) mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrot
    Matthew Thomas
    Respiratory Disease Area, Novartis Horsham Research Centre, Horsham, West Sussex, UK
    Am J Pathol 174:380-9. 2009
    ..Collectively, these data are consistent with a role for the activin receptor-like kinase 5 in the progression of idiopathic PAH and imply that strategies to inhibit activin receptor-like kinase 5 signaling may have therapeutic benefit...
  12. ncbi p65 activity and ZAP-70 status predict the sensitivity of chronic lymphocytic leukemia cells to the selective IkappaB kinase inhibitor BMS-345541
    Mónica López-Guerra
    Authors Affiliations Hematopathology Unit, Department of Pathology and Department of Hematology, Hospital Clinic, Institut d Investigacions Biomediques August Pi i Sunyer, University of Barcelona, Barcelona, Spain
    Clin Cancer Res 15:2767-76. 2009
    ..Our purpose was to characterize the molecular mechanisms underlying for the selective IkappaB kinase inhibitor BMS-345541 in CLL cells together with the analysis of its combination with several antineoplasic drugs...
  13. ncbi The growth factor response in ischemic rat retina and superior colliculus after brimonidine pre-treatment
    Ulrika Lönngren
    Department of Neuroscience, Uppsala University, Uppsala, Sweden
    Brain Res Bull 71:208-18. 2006
    ....
  14. ncbi A double-blind randomized placebo-controlled pilot study of neuropsychiatric adverse events in abstinent smokers treated with varenicline or placebo
    Dahlia Garza
    Pfizer Pharmaceuticals Inc, New York, New York 10017, USA
    Biol Psychiatry 69:1075-82. 2011
    ..There have been spontaneous postmarketing reports of neuropsychiatric adverse events (NPAEs) in smokers without a history of psychiatric illness quitting with varenicline...
  15. pmc Blockade of class IB phosphoinositide-3 kinase ameliorates obesity-induced inflammation and insulin resistance
    Naoki Kobayashi
    Department of Metabolic Diseases, Graduate School of Medicine, and Translational Systems Biology and Medicine Initiative, University of Tokyo, Tokyo 113 0033, Japan
    Proc Natl Acad Sci U S A 108:5753-8. 2011
    ..These data suggest that PI3Kγ plays a crucial role in the development of both obesity-induced inflammation and systemic insulin resistance and that PI3Kγ can be a therapeutic target for type 2 diabetes...
  16. ncbi Pharmacogenetics of smoking cessation therapy
    Gustavo L Kortmann
    Departamento de Genetica, Instituto de Biociencias, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil
    Am J Med Genet B Neuropsychiatr Genet 153:17-28. 2010
    ..However, the current scientific evidence still does not support the use of pharmacogenetic tests in routine smoking cessation therapy...
  17. pmc Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors
    Stanley F Barnett
    Department of Cancer Research, Merck and Company, Sumneytown Pike, West Point, PA 19454, USA
    Biochem J 385:399-408. 2005
    ....
  18. pmc Activation of alpha4* nAChRs is necessary and sufficient for varenicline-induced reduction of alcohol consumption
    Linzy M Hendrickson
    Brudnick Neuropsychiatric Research Institute, and Program in Neuroscience, University of Massachusetts Medical School, 303 Belmont Street, Worcester, MA 01604, USA
    J Neurosci 30:10169-76. 2010
    ..Together, our data indicate that activation of alpha4* nAChRs is necessary and sufficient for varenicline reduction of alcohol consumption...
  19. ncbi Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805
    Fabienne Baffert
    Disease Area Oncology, Novartis Institutes for BioMedical Research, 4057 Basel, Switzerland
    Mol Cancer Ther 9:1945-55. 2010
    ..Furthermore, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats...
  20. pmc Varenicline and suicidal behaviour: a cohort study based on data from the General Practice Research Database
    D Gunnell
    University of Bristol, Department of Social Medicine, University of Bristol, Bristol BS8 2PS
    BMJ 339:b3805. 2009
    ..To determine whether varenicline, a recently licensed smoking cessation product, is associated with an increased risk of suicide and suicidal behaviour compared with alternative treatments bupropion and nicotine replacement therapy...
  21. ncbi Up-regulation of brain-derived neurotrophic factor expression by brimonidine in rat retinal ganglion cells
    Hua Gao
    Department of Ophthalmology, Indiana University School of Medicine, Indianapolis, USA
    Arch Ophthalmol 120:797-803. 2002
    ..We tested the hypothesis that a possible mechanism of brimonidine neuroprotection is through up-regulation of endogenous BDNF expression in the RGCs...
  22. ncbi Differential roles of NR2A and NR2B-containing NMDA receptors in cortical long-term potentiation and long-term depression
    Peter V Massey
    Medical Research Council Centre for Synaptic Plasticity, Department of Anatomy, University of Bristol, Bristol BS8 1TD, United Kingdom
    J Neurosci 24:7821-8. 2004
    ..Therefore, NMDARs with different synaptic locations and subunit compositions are involved in various forms of synaptic plasticity in adult cortex...
  23. ncbi Complete sequence of biosynthetic gene cluster responsible for producing triostin A and evaluation of quinomycin-type antibiotics from Streptomyces triostinicus
    Alex P Praseuth
    Dept Pharmacology and Pharmaceutical Sciences, University of Southern California, Los Angeles, CA 90033, USA
    Biotechnol Prog 24:1226-31. 2008
    ..Our observation suggests potential value in careful re-analysis for metabolites from previously characterized natural product producers with the current technologies...
  24. ncbi Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization
    Stefania Butini
    European Research Centre for Drug Discovery and Development, 53100 Siena, Italy
    J Med Chem 52:6946-50. 2009
    ..In von Bezold-Jarisch reflex test 3a-c were partial agonists while 3i was a full agonist. Preliminary pharmacokinetic studies indicated that 3a is a brain penetrating agent...
  25. ncbi Selective subunit antagonists suggest an inhibitory relationship between NR2B and NR2A-subunit containing N-methyl-D: -aspartate receptors in hippocampal slices
    Andrew P Mallon
    Institute of Biomedical and Life Sciences, Division of Neuroscience and Biomedical Systems, West Medical Building, University of Glasgow, Glasgow
    Exp Brain Res 162:374-83. 2005
    ..Endogenous factors or drugs that modify this NR2B/NR2A interaction could have a major influence on synaptic transmission and plasticity in the brain...
  26. pmc Population pharmacokinetic analysis of varenicline in adult smokers
    Patanjali Ravva
    Global Pharmacometrics, Primary Care Business Unit, Worldwide Pharmaceutical Operations, Pfizer Inc, New London, Connecticut 06320, USA
    Br J Clin Pharmacol 68:669-81. 2009
    ..To characterize the population pharmacokinetics of varenicline and identify factors leading to its exposure variability in adult smokers...
  27. pmc Phase 3 randomized 3-month trial with an ongoing 3-month safety extension of fixed-combination brinzolamide 1%/brimonidine 0.2%
    Quang H Nguyen
    Scripps Clinic, La Jolla, CA 92037, USA
    J Ocul Pharmacol Ther 29:290-7. 2013
    ..2% (BBFC) with that of its component medications, brinzolamide and brimonidine, in patients with open-angle glaucoma or ocular hypertension...
  28. ncbi Neuroprotective effects of alpha(2)-selective adrenergic agonists against ischemia-induced retinal ganglion cell death
    M P Lafuente
    , , Facultad de Medicina, Universidad de Murcia, Spain
    Invest Ophthalmol Vis Sci 42:2074-84. 2001
    ..CONCLUSIONS: Pretreatment and early posttreatment with an alpha(2)-SA induces marked long-lasting neuroprotective in vivo protection against ischemia-induced cell death in RGCs...
  29. pmc A randomized placebo-controlled trial of varenicline for smoking cessation allowing flexible quit dates
    Stephen Rennard
    Division of Pulmonary, Critical Care, Sleep and Allergy, University of Nebraska Medical Center, Omaha, NE 68198 5910, USA
    Nicotine Tob Res 14:343-50. 2012
    ..The objective of this study was to compare varenicline 1 mg twice daily (b.i.d.) with placebo in subjects using a flexible quit date paradigm after starting medication...
  30. ncbi Identification and stereochemical assignment of the beta-hydroxytryptophan intermediate in the echinomycin biosynthetic pathway
    Kento Koketsu
    Division of Chemistry, Graduate School of Science, Hokkaido University, Sapporo 060 0810, Japan
    Org Lett 8:4719-22. 2006
    ....
  31. ncbi Effect of varenicline and bupropion SR on craving, nicotine withdrawal symptoms, and rewarding effects of smoking during a quit attempt
    Robert West
    Cancer Research UK Health Behaviour Unit, Department of Epidemiology and Public Health, University College London, Brook House, London, UK
    Psychopharmacology (Berl) 197:371-7. 2008
    ....
  32. ncbi Neuropsychiatric events in varenicline and nicotine replacement patch users in the Military Health System
    Tamra E Meyer
    Department of the Army, Office of the Surgeon General, Pharmacovigilance Center, Falls Church, VA 22042 5142, USA
    Addiction 108:203-10. 2013
    ..To determine the rate ratio of neuropsychiatric hospitalizations in new users of varenicline compared to new users of nicotine replacement therapy (NRT) patch in the Military Health System (MHS)...
  33. ncbi Use of varenicline for 4 weeks before quitting smoking: decrease in ad lib smoking and increase in smoking cessation rates
    Peter Hajek
    United Kingdom Centre for Tobacco Control Studies, Wolfson Institute of Preventive Medicine, Barts and the London School of Medicine and Dentistry, Queen Mary, University of London, London, England
    Arch Intern Med 171:770-7. 2011
    ..We set out to determine whether increasing the prequit medication period renders cigarettes less satisfying and facilitates quitting...
  34. ncbi Equilibrium constants for (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077) acting at recombinant NR1/NR2A and NR1/NR2B N-methyl-D-aspartate receptors: Implications for studies of sy
    Pamela A Frizelle
    Centre for Neuroscience Research, University of Edinburgh, 1 George Square, Edinburgh EH8 9JZ, UK
    Mol Pharmacol 70:1022-32. 2006
    ....
  35. pmc Varenicline is a potent agonist of the human 5-hydroxytryptamine3 receptor
    S C R Lummis
    Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1QW, United Kingdom
    J Pharmacol Exp Ther 339:125-31. 2011
    ..Therefore, activation of human 5-HT(3) receptors may be responsible for some of the side effects that preclude use of higher doses during varenicline treatment...
  36. ncbi Tobacco dependence treatment for hospitalized smokers: a randomized, controlled, pilot trial using varenicline
    Michael B Steinberg
    Division of General Internal Medicine, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School, 125 Paterson Street, Suite 2304, New Brunswick, NJ 08903, USA
    Addict Behav 36:1127-32. 2011
    ..This is the first randomized, double-blinded, placebo-controlled pilot trial utilizing varenicline and post-discharge, in-person behavioral treatment for hospitalized smokers...
  37. pmc The safety and efficacy of varenicline in cocaine using smokers maintained on methadone: a pilot study
    James Poling
    Yale University School of Medicine, VA Connecticut Healthcare System, West Haven, Connecticut 06516, USA
    Am J Addict 19:401-8. 2010
    ..These preliminary findings may point to potential therapeutic value of varenicline for smoking cessation in cocaine users maintained on methadone...
  38. ncbi Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice
    Xiao dong Peng
    State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan, China
    J Pharmacol Exp Ther 332:46-56. 2010
    ....
  39. pmc Brimonidine blocks glutamate excitotoxicity-induced oxidative stress and preserves mitochondrial transcription factor a in ischemic retinal injury
    Dongwook Lee
    The Sophie and Arthur Laboratory for Optic Nerve Biology, Hamilton Glaucoma Center, University of California San Diego, La Jolla, United States of America
    PLoS ONE 7:e47098. 2012
    ..Our findings suggest that systemic BMD treatment protects RGCs by blockade of glutamate excitotoxicity-induced oxidative stress and subsequent preservation of Tfam/OXPHOS complex expression in ischemic retina...
  40. ncbi Phosphoinositol 3-kinase-gamma mediates antineutrophil cytoplasmic autoantibody-induced glomerulonephritis
    Adrian Schreiber
    Department of Nephrology and Hypertension, Medical Faculty of the Charite, Franz Volhard Clinic, Max Delbruck Center for Molecular Medicine, Schwanebecker Chaussee 50, Berlin, Germany
    Kidney Int 77:118-28. 2010
    ..We found that PI3Kgamma plays a pivotal role in ANCA-induced NCGN and suggest that its specific inhibition may provide a novel treatment target...
  41. pmc Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor
    Karen Coopman
    Department of Cell Physiology and Pharmacology, University of Leicester, Leicester, United Kingdom
    J Pharmacol Exp Ther 334:795-808. 2010
    ..Full assessment of the properties of compound 2 was potentially hampered by damaging effects that were particularly manifest in either longer term assays with intact cells or in acute assays with membranes...
  42. ncbi An update on therapeutics for tobacco dependence
    Tim Lancaster
    University of Oxford, Cochrane Tobacco Addiction Review Group, Department of Primary Healthcare, Old Road, Headington, Oxford, OX3 7LF, UK
    Expert Opin Pharmacother 9:15-22. 2008
    ..Recent evidence suggests that the nicotine-receptor partial agonist varenicline is at least as effective as nicotine replacement therapy and antidepressants...
  43. ncbi Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core
    N Armstrong
    Department of Biochemistry and Molecular Biophysics, Columbia University, New York, New York 10032, USA
    Neuron 28:165-81. 2000
    ..The crystal packing of the ligand binding cores suggests modes for subunit-subunit contact in the intact receptor and mechanisms by which allosteric effectors modulate receptor activity...
  44. pmc A preliminary investigation of varenicline for heavy drinking smokers
    Lisa M Fucito
    Department of Psychiatry, CMHC S200, Yale University School of Medicine, 34 Park Street, New Haven, CT 06519, USA
    Psychopharmacology (Berl) 215:655-63. 2011
    ..However, varenicline has not been tested in heavy drinkers, and it remains to be determined whether varenicline could reduce alcohol craving and consumption in smokers who are trying to quit smoking...
  45. ncbi Alpha-2 adrenoceptor agonist protects retinal function after acute retinal ischemic injury in the rat
    Ronald K Lai
    Department of Biological Sciences, Allergan, Inc, Irvine, CA 92612, USA
    Vis Neurosci 19:175-85. 2002
    ..All these aforementioned factors may potentially contribute in mediating brimonidine's protective effect in this acute retinal ischemia model...
  46. ncbi Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro
    R Scott Obach
    Department of Pharmacokinetics, Dynamics, and Drug Metabolism, Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA
    Drug Metab Dispos 34:121-30. 2006
    ..The straightforward dispositional profile of varenicline should simplify its use in the clinic as an aid in smoking cessation...
  47. pmc Electric fields due to synaptic currents sharpen excitatory transmission
    Sergiy Sylantyev
    Institute of Neurology, University College London, Queen Square, London, WC1N 3BG, UK
    Science 319:1845-9. 2008
    ..Voltage-dependent temporal tuning of excitatory synaptic responses may thus contribute to signal integration in neural circuits...
  48. pmc Ethanol facilitates glutamatergic transmission to dopamine neurons in the ventral tegmental area
    Cheng Xiao
    Department of Anesthesiology, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Newark, NJ 07103, USA
    Neuropsychopharmacology 34:307-18. 2009
    ..Enhancement of this positive feedback loop may significantly contribute to the development of alcohol addiction...
  49. ncbi Combination treatment with varenicline and nicotine replacement therapy
    Jon O Ebbert
    Mayo Clinic College of Medicine, 200 1st Street Southwest, Rochester, MN 55905, USA
    Nicotine Tob Res 11:572-6. 2009
    ..A paucity of data exists regarding the safety and effectiveness of combination treatment with varenicline and nicotine replacement therapy (NRT)...
  50. pmc Emotional environments retune the valence of appetitive versus fearful functions in nucleus accumbens
    Sheila M Reynolds
    Department of Psychology, 525 E University Avenue, University of Michigan, Ann Arbor, Michigan 48109 1109, USA
    Nat Neurosci 11:423-5. 2008
    ..Thus, the emotional environments retuned the generation of motivation in corticolimbic circuits...
  51. pmc Pharmacology of nicotine: addiction, smoking-induced disease, and therapeutics
    Neal L Benowitz
    Department of Medicine, Division of Clinical Pharmacology and Experimental Therapeutics, Medical Service, San Francisco General Hospital Medical Center, University of California, San Francisco, California 94143 1220, USA
    Annu Rev Pharmacol Toxicol 49:57-71. 2009
    ..Pharmacotherapeutic approaches to tobacco addiction include nicotine replacement, bupropion, and varenicline, the latter a selective nicotine receptor partial agonist...
  52. ncbi Differential roles of NR2A and NR2B-containing NMDA receptors in LTP and LTD in the CA1 region of two-week old rat hippocampus
    Thomas E Bartlett
    MRC Centre for Synaptic Plasticity, Department of Anatomy, University of Bristol, School of Medical Sciences, University Walk, Bristol, BS8 1TD, UK
    Neuropharmacology 52:60-70. 2007
    ..4 microM. The lack of effect of 0.1 microM NVP on LTD contrasts with its marked effect on LTP and raises the possibility that different NVP-sensitive NR2 subunit-containing NMDA receptors are required for LTP and LTD in this preparation...
  53. ncbi A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice
    Kim W McIntyre
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    Arthritis Rheum 48:2652-9. 2003
    ....
  54. ncbi Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trial
    David Gonzales
    Smoking Cessation Center, Department of Medicine, Oregon Health and Science University, Portland, OR 97239, USA
    JAMA 296:47-55. 2006
    ..The alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are linked to the reinforcing effects of nicotine and maintaining smoking behavior. Varenicline, a novel alpha4beta2 nAChR partial agonist, may be beneficial for smoking cessation...
  55. pmc Early alterations of AMPA receptors mediate synaptic potentiation induced by neonatal seizures
    Sanjay N Rakhade
    Department of Neurology, Division of Neuroscience, Children s Hospital, Boston, Massachusetts 02115, USA
    J Neurosci 28:7979-90. 2008
    ..Thus, the potentiation of AMPAR-containing synapses is a reversible, early step in epileptogenesis that offers a novel therapeutic target in the highly seizure-prone developing brain...
  56. ncbi Functional cross-talk between fatty acid synthesis and nonribosomal peptide synthesis in quinoxaline antibiotic-producing streptomycetes
    Gernot Schmoock
    Institut fur Chemie, Arbeitsgruppe Biochemie und Molekularbiologie, Technische Universitat Berlin, Franklinstrasse 29, D 10587 Berlin Charlottenburg, Germany
    J Biol Chem 280:4339-49. 2005
    ..These data show for the first time a functional interaction between nonribosomal peptide synthesis and fatty acid synthesis...
  57. pmc Definitive role for natriuretic peptide receptor-C in mediating the vasorelaxant activity of C-type natriuretic peptide and endothelium-derived hyperpolarising factor
    Inmaculada C Villar
    Clinical Pharmacology, William Harvey Research Institute, Bart s and The London, Charterhouse Square, London EC1M 6BQ, UK
    Cardiovasc Res 74:515-25. 2007
    ....
  58. ncbi Substrate specificity of the OqxAB multidrug resistance pump in Escherichia coli and selected enteric bacteria
    Lars Hestbjerg Hansen
    Department of Microbiology, Institute of Biology, University of Copenhagen, Sølvgade 83H, 1307 Copenhagen K, Denmark
    J Antimicrob Chemother 60:145-7. 2007
    ..The ability of horizontal transfer to food-borne pathogens of the Enterobacteriaceae family was also investigated...
  59. ncbi Lack of NMDA receptor subtype selectivity for hippocampal long-term potentiation
    Sven Berberich
    Department of Molecular Neurobiology, Max Planck Institute for Medical Research, D 69120 Heidelberg, Germany
    J Neurosci 25:6907-10. 2005
    ....
  60. ncbi Effect of acute and chronic treatment with QCF-3 (4-benzylpiperazin-1-yl) (quinoxalin-2-yl) methanone, a novel 5-HT(3) receptor antagonist, in animal models of depression
    Thangaraj Devadoss
    Pharmacy Group, FD III, Birla Institute of Technology and Science, Pilani, Rajasthan 333031, India
    Pharmacol Rep 62:245-57. 2010
    ..In conclusion, this behavioral study describes an antidepressant-like effect of QCF-3 in rodent behavioral models of depression...
  61. ncbi Adverse effects and tolerability of medications for the treatment of tobacco use and dependence
    J Taylor Hays
    Mayo Clinic Nicotine Dependence Center, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA
    Drugs 70:2357-72. 2010
    ..Given these factors, the benefit : risk ratio is strongly in favour of pharmacotherapy for tobacco dependence treatment in virtually all smokers who are motivated to quit...
  62. ncbi Psychiatric adverse events associated with varenicline: an intensive postmarketing prospective cohort study in New Zealand
    Mira Harrison-Woolrych
    Intensive Medicines Monitoring Programme, Department of Preventive and Social Medicine, University of Otago, Dunedin, New Zealand
    Drug Saf 34:763-72. 2011
    ..However, data regarding the frequency of psychiatric adverse reactions in 'real-life' postmarketing use are limited to date...
  63. ncbi Cardiovascular events in patients taking varenicline: a case series from intensive postmarketing surveillance in New Zealand
    Mira Harrison-Woolrych
    Intensive Medicines Monitoring Programme, New Zealand Pharmacovigilance Centre, Department of Preventive and Social Medicine, University of Otago Medical School, Dunedin, New Zealand
    Drug Saf 35:33-43. 2012
    ..Cases of cardiovascular events, including myocardial infarction (MI) and cardiac dysrhythmias, have been noted from spontaneous reporting systems...
  64. pmc Conjugative plasmid conferring resistance to olaquindox
    Anders Hay Sørensen
    Department of General Microbiology, University of Copenhagen, 1307 Copenhagen K, Denmark
    Antimicrob Agents Chemother 47:798-9. 2003
    ..It also confers resistance to ampicillin and chloramphenicol and has a high frequency of transfer between strains of E. coli. Plasmid-borne olaquindox resistance has not been demonstrated before...
  65. ncbi The smoking cessation medication varenicline attenuates alcohol and nicotine interactions in the rat mesolimbic dopamine system
    Mia Ericson
    Institute of Neuroscience and Physiology, the Sahlgrenska Academy at University of Gothenburg, Gothenburg, Sweden
    J Pharmacol Exp Ther 329:225-30. 2009
    ....
  66. ncbi Varenicline: a pharmacoeconomic review of its use as an aid to smoking cessation
    Gillian M Keating
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Pharmacoeconomics 28:231-54. 2010
    ....
  67. ncbi The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study
    M R Walters
    University Department of Medicine and Therapeutics, Western Infirmary, Glasgow, UK
    Cerebrovasc Dis 20:304-9. 2005
    ..It has demonstrated neuroprotective efficacy in experimental models of stroke and tolerability in healthy volunteers. We tested the safety and tolerability of ZK 200775 in patients with acute ischaemic stroke...
  68. ncbi Possible neuroprotective effect of brimonidine in a mouse model of ischaemic optic neuropathy
    Nitza Goldenberg-Cohen
    Pediatric Division of Ophthalmology, Schneider Children s Medical Center of Israel, Tel Aviv, Israel
    Clin Experiment Ophthalmol 37:718-29. 2009
    ..To investigate the neuroprotective effect of brimonidine following induction of ischaemic optic neuropathy in rodents (rAION)...
  69. ncbi Varenicline treatment for smoking cessation in Asian populations: a pooled analysis of placebo-controlled trials conducted in six Asian countries
    Karl Fagerström
    Smokers Information Centre, Fagerstrom Consulting AB, Helsingborg, Sweden
    Curr Med Res Opin 26:2165-73. 2010
    ..A pooled analysis to evaluate the efficacy and safety of varenicline versus placebo for smoking cessation in Asian populations. A secondary objective was to compare the data to pooled trials among predominantly Western populations...
  70. ncbi Developmental changes in NMDA neurotoxicity reflect developmental changes in subunit composition of NMDA receptors
    MiOu Zhou
    Neuroscience Program, University of Southern California, Los Angeles, California 90089 2520, USA
    J Neurosci 26:2956-63. 2006
    ....
  71. pmc Behavioral counseling and varenicline treatment for smoking cessation
    Gary E Swan
    SRI International, Menlo Park, California 94025, USA
    Am J Prev Med 38:482-90. 2010
    ..Smoking remains the primary preventable cause of death and illness in the U.S. Effective, convenient treatment programs are needed to reduce smoking prevalence...
  72. ncbi Clinical signs and performance of pigs treated with different doses of carbadox, cyadox and olaquindox
    M J Nabuurs
    Centraal Diergeneeskundig Instituut, Central Veterinary Institute, Lelystad, The Netherlands
    Zentralbl Veterinarmed A 37:68-76. 1990
    ..From this study one may conclude that, within the dosages used, carbadox is more harmful than olaquindox for pigs, and it seems that cyadox is harmless for pigs in dosages up to 400 ppm...
  73. ncbi Spinal AMPA receptor inhibition attenuates mechanical allodynia and neuronal hyperexcitability following spinal cord injury in rats
    Young Seob Gwak
    Department of Physiology, Brain Research Institute, and BK21 Project for Medical Science, Yonsei University College of Medicine, Seoul, Korea
    J Neurosci Res 85:2352-9. 2007
    ..In conclusion, our study demonstrates that the AMPA receptor plays an important role in behaviors related to the maintenance of central neuropathic pain below the level of spinal cord injury...
  74. ncbi Delayed antagonism of AMPA/kainate receptors reduces long-term functional deficits resulting from spinal cord trauma
    J R Wrathall
    Department of Cell Biology, Georgetown University, Washington, DC 20007, USA
    Exp Neurol 145:565-73. 1997
    ..Further, they suggest the intriguing hypothesis that mechanisms underlying early functional recovery after SCI are, at least in part, distinct those from those involved in reducing chronic functional deficits...
  75. ncbi Apoptosis and anti-apoptosis signalling in glaucomatous retinopathy
    W G Tatton
    Department of Ophthalmology, Mount Sinai Medical Center, New York, New York 10029, USA
    Eur J Ophthalmol 11:S12-22. 2001
    ....
  76. ncbi Neuroprotective effect of alpha(2) agonist (brimonidine) on adult rat retinal ganglion cells after increased intraocular pressure
    F A Ahmed
    Department of Ophthalmology, New York Medical College, Valhalla, NY 10595, USA
    Brain Res 913:133-9. 2001
    ..Although pressure remained elevated throughout the length of the experiment, 3 weeks later the amount of cell death gradually increased in brimonidine-treated animals...
  77. ncbi Effects of varenicline on smoking cessation in patients with mild to moderate COPD: a randomized controlled trial
    Donald P Tashkin
    Department of Medicine, David Geffen School of Medicine at University of California, Los Angeles, 10833 Le Conte Ave, Los Angeles, CA 90095 1690, USA
    Chest 139:591-9. 2011
    ..To our knowledge, this is the first randomized clinical trial to compare the efficacy and safety of varenicline tartrate vs placebo in smokers with mild to moderate COPD...
  78. ncbi Varenicline-associated acute renal failure
    Matthew L Bird
    Department of Pharmacy, Clinical Administrative Sciences, College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73117, USA
    Ann Pharmacother 42:1908-11. 2008
    ..To report an association between acute renal failure and varenicline...
  79. ncbi Design, synthesis and structure-activity relationship of novel quinoxalin-2-carboxamides as 5-HT3 receptor antagonists for the management of depression
    Radhakrishnan Mahesh
    Pharmacy Group, FD III, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, India
    Bioorg Med Chem Lett 20:6773-6. 2010
    ..Compounds with significant pA(2) values exhibited good anti-depressant-like activity as compared to the vehicle-treated group...
  80. ncbi Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors
    Emanuele Carosati
    Dipartimento di Chimica, Universita degli Studi di Perugia, Via Elce di Sotto 10, 06123 Perugia, Italy
    Bioorg Med Chem 18:7773-85. 2010
    ..Previously, two quinoxalines have been identified as inhibitors of the folate-dependent proteins belonging to the thymidylate synthase cycle...
  81. ncbi The mechanism of enzymatic and non-enzymatic N-oxide reductive metabolism of cyadox in pig liver
    Ming Zheng
    College of Life Sciences, South China Agricultural University, Guangzhou 510642, China
    Xenobiotica 41:964-71. 2011
    ..The research provides a basic foundation for the formulation of safety controls for animal products and the properties and metabolism of heterocyclic N-oxides...
  82. ncbi Pharmacokinetics, safety, and tolerability after single and multiple oral doses of varenicline in elderly smokers
    Aaron H Burstein
    Department of Medical and Developmental Sciences, Pfizer Global Research and Development, Groton New London Labs, MS8260 2505, Groton, CT 06340, USA
    J Clin Pharmacol 46:1234-40. 2006
    ..Varenicline was well tolerated; all adverse events reported were mild to moderate in intensity. Thus, no dose adjustment is necessary based on age alone...
  83. ncbi [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists
    Hilde Lavreysen
    CNS Discovery Research, Johnson and Johnson Pharmaceutical Research and Development, Beerse, Belgium
    Mol Pharmacol 63:1082-93. 2003
    ..The high affinity and selectivity of [(3)H]R214127 for mGlu1 receptors renders this compound the ligand of choice to study the native mGlu1 receptor in brain...
  84. pmc A pilot study of the efficacy of varenicline for the treatment of smokeless tobacco users in Midwestern United States
    Jon O Ebbert
    Mayo Clinic College of Medicine, Rochester, MN 55905, USA
    Nicotine Tob Res 13:820-6. 2011
    ..We have conducted a pilot study to obtain preliminary evidence of efficacy of varenicline for the treatment of ST users in Midwestern United States...
  85. ncbi Synthesis, analytical behaviour and biological evaluation of new 4-substituted pyrrolo[1,2-a]quinoxalines as antileishmanial agents
    Jean Guillon
    EA 2962 Pharmacochimie, UFR des Sciences Pharmaceutiques, Universite Victor Segalen Bordeaux 2, 146 rue Leo Saignat, 33076 Bordeaux Cedex, France
    Bioorg Med Chem 15:194-210. 2007
    ..Structure-activity relationships enlighten the importance of the 4-substituted alkenyl side chain on the pyrrolo[1,2-a]quinoxaline moiety to modulate the antileishmanial activity...
  86. ncbi Effects of varenicline in adult smokers: a multinational, 24-week, randomized, double-blind, placebo-controlled study
    Chris T Bolliger
    Respiratory Research Unit, Faculty of Health Sciences, University of Stellenbosch, Cape Town, South Africa
    Clin Ther 33:465-77. 2011
    ..Prevalence rates of smoking are rising in developing countries. Previous trials evaluating the efficacy and tolerability of the smoking-cessation medication varenicline have used largely participants of Caucasian origin...
  87. ncbi Q39, a novel synthetic Quinoxaline 1,4-Di-N-oxide compound with anti-cancer activity in hypoxia
    Qinjie Weng
    Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
    Eur J Pharmacol 581:262-9. 2008
    ..The mitochondrial pathway mediated by Bcl-2 protein family and MAPKs and the HIF-1 pathway might be involved in signaling Q39-induced apoptosis...
  88. ncbi The efficacy and safety of varenicline for smoking cessation using a flexible dosing strategy in adult smokers: a randomized controlled trial
    Raymond Niaura
    Brown University, Providence, RI, USA
    Curr Med Res Opin 24:1931-41. 2008
    ..To determine whether self-regulated flexible dosing with varenicline tartrate is safe and effective for smoking cessation...
  89. ncbi Long-lasting synaptic modification in the rat hippocampus resulting from NMDA receptor blockade during development
    Frederick P Bellinger
    Alcohol Research Unit, Department of Biochemistry, The University of Queensland, St Lucia, QLD 4072, Australia
    Synapse 43:95-101. 2002
    ..Glutamate receptor antagonism did not produce lasting changes in long-term potentiation or paired-pulse facilitation. These results indicate activation of NMDA receptors during development is necessary for proper development of synapses...
  90. ncbi Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently
    Ye Hwang Cheong
    Research Center, Dong A Pharmaceuticals Co Ltd, Giheung gu, Yongin si, Gyeonggi Do, Republic of Korea
    Biochem Biophys Res Commun 417:558-63. 2012
    ..Taken together, our findings suggest that compounds 2 and B have different modes of action to activate GLP-1R. Further study to identify the putative binding sites will help in the discovery of orally available GLP-1R agonists...
  91. pmc Smoking outcome by psychiatric history after behavioral and varenicline treatment
    Jennifer B McClure
    Group Health Research Institute, Seattle, WA 98101, USA
    J Subst Abuse Treat 38:394-402. 2010
    ..Groups had similar 30-day abstinence rates at 6 months (31.5% PH+ vs. 35.4% PH-, p = .35). In sum, having a psychiatric diagnosis in this trial did not predict worse treatment outcome or worse treatment side effects...
  92. pmc Pharmacotherapies for smoking cessation: a meta-analysis of randomized controlled trials
    Mark J Eisenberg
    Division of Cardiology and Clinical Epidemiology, Sir Mortimer B Davis Jewish General Hospital and McGill University, McGill University, Montreal, QC
    CMAJ 179:135-44. 2008
    ..However, few direct or indirect comparisons of such interventions have been conducted. We performed a meta-analysis to compare the treatment effects of 7 approved pharmacologic interventions for smoking cessation...
  93. ncbi [Intervention effect of PI3Kgamma inhibitor AS605240 on autoimmune myocarditis in mice]
    Ke Jin
    State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, China
    Sichuan Da Xue Xue Bao Yi Xue Ban 40:817-20, 825. 2009
    ..To investigate the therapeutic effect of PI3Kgamma inhibitor AS605240 on autoimmune myocarditis in mice...
  94. ncbi Subchronic oral toxicity study with cyadox in Wistar rats
    Guijie Fang
    National Reference Laboratory of Veterinary Drug Residues and MOA Key Laboratory of Food Safety Evaluation, Huazhong Agricultural University, Wuhan, Hubei, PR China
    Food Chem Toxicol 44:36-41. 2006
    ..It was for the first time that changes were found in the liver and kidneys of rats fed 2500 mg/kg cyadox. The no-observed-adverse-effect level (NOAEL) of cyadox for rats was estimated to be 150 mg/kg dietary dose level...
  95. ncbi Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents
    A D Andricopulo
    College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109 1065, USA
    Bioorg Med Chem Lett 16:2283-92. 2006
    ..Furthermore, all three compounds were active in the lower micromolar range on the chloroquine-resistant P. falciparum strain K1 in vitro...
  96. ncbi Olaquindox-induced genotoxicity and oxidative DNA damage in human hepatoma G2 (HepG2) cells
    Jiajie Zou
    Department of Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing 100193, PR China
    Mutat Res 676:27-33. 2009
    ..Considering all the results, it is inferred that olaquindox exerts genotoxic effects in HepG2 cells probably through the ROS-induced oxidative DNA damage...
  97. ncbi Effects of cyadox and olaquindox on intestinal mucosal immunity and on fecal shedding of Escherichia coli in piglets
    M X Ding
    National Reference Laboratory of Veterinary Drug Residues, MOA Key Laboratory of Food Safety Evaluation, Huazhong Agricultural University, Wuhan 430070, People s Republic of China
    J Anim Sci 84:2367-73. 2006
    ..The data indicated that olaquindox and cyadox reduced the number of intestinal E. coli and suppressed E. coli-induced immune activation, which might be responsible for the enhanced growth that was observed...
  98. ncbi Synthesis and in vitro antitumor activity of new quinoxaline derivatives
    Paola Corona
    Dipartimento Farmaco Chimico Tossicologico, Universita degli Studi di Sassari, Via Muroni 23 A, 07100 Sassari, Italy
    Eur J Med Chem 44:1579-91. 2009
    A series of novel 5,7-diamino-3-phenyl-2-benzylamino, 2-phenoxy, and 2-thiophenyl substituted quinoxalines has been designed, synthesized and evaluated for their in vitro antitumor activity towards cell lines of nine different types of ..
  99. ncbi Silica bonded S-sulfonic acid: a recyclable catalyst for the synthesis of quinoxalines at room temperature
    Khodabakhsh Niknam
    Department of Chemistry, Faculty of Sciences, Persian Gulf University, Bushehr, Iran
    Molecules 14:1915-26. 2009
    ..The catalyst could be recycled and reused several times without any loss of efficiency...
  100. pmc A phase I and pharmacokinetic study of the quinoxaline antitumour Agent R(+)XK469 in patients with advanced solid tumours
    Samir D Undevia
    Department of Medicine, Section of Hematology Oncology, University of Chicago, Chicago, IL 60637, USA
    Eur J Cancer 44:1684-92. 2008
    ..Preclinical studies suggested that efficacy was independent of schedule but that toxicity was decreased by dividing the dose...
  101. ncbi Design and synthesis of novel 7-heterocycle-6-trifluoromethyl-3-oxoquinoxaline-2-carboxylic acids bearing a substituted phenyl group as superior AMPA receptor antagonists with good physicochemical properties
    Yasuo Takano
    Discovery Research Laboratories, Kyorin Pharmaceutical Co, Ltd, 2399 1, Nogi, Nogi machi, Simotsuga gun, Tochigi 329 0114, Japan
    Bioorg Med Chem 14:776-92. 2006
    ..Furthermore, the compound showed good physicochemical properties, including stability to light and good solubility in aqueous solutions...

Research Grants68

  1. High Dose Nicotine Patch Therapy for Spit Tobacco Users
    Jon Ebbert; Fiscal Year: 2004
    ..Our goal is to reduce the prevalence of ST use and decrease the incidence of oropharyngeal cancer through the development of effective treatment options for ST users. ..
  2. Evaluating Nicotine Lozenges for Treatment of Smokeless Tobacco Addiction
    Jon Ebbert; Fiscal Year: 2009
    ..No drug therapies have been shown to be effective for helping smokeless tobacco users quit for good. The purpose of this study is to test drugs that can be used to help smokeless tobacco users quit for good. ..
  3. Brief Dental Office Intervention with Tobacco Quitline
    Jon Ebbert; Fiscal Year: 2005
    ..S. adult population smoking; and 3) 75% of smokers quitting for at least one day or longer because they are trying to quit. ..
  4. SEX DIFFERENCES IN NICOTINE REINFORCEMENT: HUMAN/ANIMAL
    Kenneth Perkins; Fiscal Year: 2003
    ....
  5. Gradual vs Abrupt Cessation Treatment for Smoking
    John Hughes; Fiscal Year: 2007
    ..This study will be the first large, systematic test of gradual vs. abrupt cessation. ..
  6. Internal Barriers to Seeking Smoking Cessation Treatment
    John Hughes; Fiscal Year: 2007
    ..Our results will suggest messages for media campaigns and for clinicians to use to motivate smokers to access proven treatments. ..
  7. INDIVIDUAL VARIATION IN NICOTINE SENSITIVITY IN HUMANS
    Kenneth Perkins; Fiscal Year: 2003
    ..e., in nicotine-naive individuals). Results will provide directions for future research on vulnerability to tobacco dependence and for targeted efforts to prevent smoking onset. ..
  8. Tobacco Smoking, Nicotine and Negative Affect Relief
    Kenneth Perkins; Fiscal Year: 2009
    ..In sum, this research will help address the fundamental question of why cigarette smoking is reinforcing. ..
  9. Affect, Context, and Placebo Responses to Nicotine
    Kenneth Perkins; Fiscal Year: 2005
    ..Secondary analyses may identify important individual characteristics associated with placebo responses, aiding in the prediction of which smokers ultimately are likely to benefit most from manipulation of placebo effects. ..
  10. EVALUATION OF A CIGARETTE SUBSTITUTE
    John Hughes; Fiscal Year: 2001
    ..We believe it imperative to begin studying these substitutes so that, unlike low-tar/low nicotine cigarettes, we will know whether their introduction is good or bad for public health. ..
  11. Natural History of Attempts to Stop Smoking
    John R Hughes; Fiscal Year: 2010
    ....
  12. DISCRIMINATIVE STIMULUS EFFECTS OF NICOTINE
    Kenneth Perkins; Fiscal Year: 2001
    ....
  13. Novel approach to measure DNA adducts in humans
    ROBERT TURESKY; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  14. Negative Affect and Smoking Behavior in Women and Men
    Sherry McKee; Fiscal Year: 2006
    ..Ultimately, it is hoped that this model could be extended to evaluate the effect of pharmacological agents on tobacco relapse behavior. [unreadable] [unreadable]..
  15. Retinal Inputs to the Mammalian Circadian Pacemaker
    KWOON WONG; Fiscal Year: 2006
    ..These experiments may enable a better understanding of how the mammalian circadian pacemaker is regulated, which in turn may lead to better therapies and workplace policies combating/preventing jet lag problems. ..
  16. Investigating Tobacco & Alcohol Use Behaviors Across the Continuum of Use
    Sherry McKee; Fiscal Year: 2006
    ..The results generated from this application will have important clinical and public health implications, and further our understanding of alcohol-tobacco interactions. ..
  17. REGULATION OF INTRAOCULAR PRESSURE AND OCULAR BLOOD FLOW
    John Liu; Fiscal Year: 2007
    ..New knowledge of ocular blood flow and lOP in patients would have implications for the better diagnosis and treatment of glaucoma. ..
  18. Oligopyrrole-based Anion Binding Agents
    Jonathan L Sessler; Fiscal Year: 2010
    ..abstract_text> ..
  19. Smoking Cessation for Head and Neck Cancer Patients
    Robert Schnoll; Fiscal Year: 2006
    ..In turn, our findings may help guide the implementation of smoking cessation treatments for all cancer patients within Comprehensive Cancer Centers in the US. ..
  20. Bupropion for Smoking Cessation in Postpartum Women
    Nancy Rigotti; Fiscal Year: 2007
    ..If this pilot is successful, we plan to test the safety and efficacy of bupropion SR in a future full-scale randomized double-blind placebo-controlled trial for smoking cessation in postpartum women. [unreadable] [unreadable]..
  21. Biometric and Measured Genetic Research on Smoking
    Gary Swan; Fiscal Year: 2007
    ..Such knowledge will confer new insights about the etiology and progression of smoking and should improve the current understanding of smoking, which is still largely descriptive. ..
  22. ASK, ADVISE, REFER: Promoting Pharmacy-based Referrals to Tobacco Quitlines
    Karen S Hudmon; Fiscal Year: 2010
    ....
  23. Impact of Smoking Cessation on Sleep
    Gary Swan; Fiscal Year: 2008
    ..The results of this project will be particularly important for the development of targeted treatment approaches designed to ameliorate sleep disruption as part of an overall smoking cessation strategy. ..
  24. Treatment of Nicotine Dependence in Health Care Setting
    Gary Swan; Fiscal Year: 2009
    ....
  25. BLOOD PRESSURE CONTROL BY FOREBRAIN & BRAINSTEM NEURONS
    SUSAN BARMAN; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  26. Do Treatments for Smoking Cessation Reduce Alcohol Drinking?
    Sherry McKee; Fiscal Year: 2009
    ..Omg). This proposal will have important treatment implications for improving rates of smoking cessation in hazardous drinkers and will contribute to the understanding of alcohol-nicotine interactions. ..
  27. Safety of Nicotine Reduction Strategy
    Neal Benowitz; Fiscal Year: 2009
    ..The proposed research is needed to guide governmental regulators as to how best to regulate nicotine in cigarettes and is an essential first step in examining the feasibility of a national regulation program. ..
  28. Nicotine Intake in Smokers with Schizophrenia
    Jill Williams; Fiscal Year: 2009
    ....
  29. Nicotine Dependence Treatment in Psychiatric Comorbidity
    Jill Williams; Fiscal Year: 2005
    ..Techniques from dual diagnosis treatment can be adapted for treating nicotine dependence and include aspects of social skills training, motivational enhancement therapy and relapse prevention. ..
  30. BUPROPION FOR HOSPITALIZED SMOKERS W CORONARY DISEASE
    Nancy Rigotti; Fiscal Year: 2002
    ..If found to be safe and effective, bupropion SR could become a standard part of "secondary prevention" therapy for smokers with acute CHD, a large, high-risk, high-cost patient group. ..
  31. CVD RISK FACTORS AND BRAIN MORPHOLOGY IN NHLBI TWINS
    Gary Swan; Fiscal Year: 2001
    ....
  32. PHARMACOKINETICS OF NICOTINE IN TWINS
    Gary Swan; Fiscal Year: 2002
    ..Ultimately, this knowledge may lead to more informed and more finely targeted treatment of individuals who are either susceptible to nicotine addiction or are already addicted to this substance. ..
  33. Medicinal Inorganic Chemistry ACS Symposium F-2003
    Jonathan Sessler; Fiscal Year: 2003
    ..It is thus expected that the present MIC-ACS symposium will afford a unique opportunity to develop further growth in a field of study that is rich in opportunity and central to the NIH mission. ..
  34. MOLECULAR BIOLOGY OF CAMPTOTHECIN INDUCED DNA DAMAGE
    ROBERT SNAPKA; Fiscal Year: 2002
    ..abstract_text> ..
  35. Conference on Photodynamic Therapy
    David Kessel; Fiscal Year: 2002
    ..The most recent PDT meeting, sponsored by the International Photodynamic Assn, has more than 600 participants. ..
  36. Dendritic Processing in the Olfactory Bulb
    Jason Christie; Fiscal Year: 2003
    ..The specific aims are: (1) to determine the function of autoexcitation in mitral cell processing and (2) to determine how dendritic compartmentalization effects mitral cell processing. ..
  37. Alcohol Self-Administration/Effect/Nicotine Replacement
    Sherry McKee; Fiscal Year: 2003
    ..This study will have important implications for alcohol-nicotine interactions, smoking cessation in alcohol drinkers, and alcohol challenge studies in general. ..
  38. Promotion of PDT Induced phototoxicity by bile acids
    David Kessel; Fiscal Year: 2003
    ..If the results of preliminary studies are borne out by further investigation, UDCA could offer a safe and effective means for promoting clinical PDT efficacy. ..
  39. A Preclinical Chemopreventive Model in Prostate Cancer
    Kenneth Turteltaub; Fiscal Year: 2004
    ..abstract_text> ..
  40. R01-Williajm - Double-Blind Placebo-Controlled trial of Nicotine Nasal Spray as a
    Jill M Williams; Fiscal Year: 2010
    ..There is a need to systematically examine available treatments and explore new ones that can address their needs. ..
  41. PROTEOMICS OF TOPOISOMERASE-DNA CLEAVAGE COMPLEXES
    ROBERT SNAPKA; Fiscal Year: 2007
    ..abstract_text> ..
  42. Nicotine Replacement Treatment for Pregnant Smokers
    Cheryl Oncken; Fiscal Year: 2006
    ..The odds of cigarette abstinence will be increased primarily in subjects who smoke at least 15 cigarettes per day...
  43. PREVENTIVE ONCOLOGY AWARD--SMOKING CESSATION AND WOMEN
    JENNIFER MC CLURE; Fiscal Year: 2003
    ..Such knowledge is important as it may lead to the development of more targeted, and therefore potentially more effective, cessation interventions. ..
  44. Proactive Cessation Intervention with Biomarker Feedback
    JENNIFER MC CLURE; Fiscal Year: 2008
    ..If effective, this treatment strategy could have broad potential as a public health intervention. ..
  45. NICOTINE ADDICTION IN MICE LACKING THE NEURONAL NACHR
    MARINA PICCIOTTO; Fiscal Year: 2009
    ..We propose that this mouse model may have implications for the development of psychiatric disorders in subjects exposed to nicotine in utero. ..
  46. LONG TERM POTENTIATION AND DEPRESSION IN THE CEREBELLUM
    David Linden; Fiscal Year: 2002
    ..In addition, these investigations have potential clinical relevance not only for cerebellar motor disorders, but also for disorders of learning and memory generally. ..
  47. SCHEDULED SMOKING WITH TRANSDERMAL NICOTINE
    Paul Cinciripini; Fiscal Year: 2001
    ..We hypothesize that smokers receiving the combined treatment (SSNP) will be abstinent more often, and show greater changes in coping and other behaviors, than smokers in either the SS or NP groups. ..
  48. MECHANISMS OF WATER TRANSPORT IN RENAL EPITHELIA
    Alan Verkman; Fiscal Year: 2008
    ..Methods will include fluorescence photobleaching recovery, energy transfer and ratio imaging. Also, specific water/solute transporting properties (Pd, c^)of the mammalian aquaporins will be measured. ..
  49. PURINERGIC AXIS OF CARDIAC BLOOD VESSELS
    IAIN BUXTON; Fiscal Year: 2001
    ..We will approach these aims with biochemical, pharmacological, molecular, cell biological and microscopic methods employing intact blood vessels, cells in primary culture and subcellular fractions. ..
  50. Cellular Plasticity Following Repeated Amphetamine
    Christopher Nelson; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  51. STRESS AND THE NEUROBIOLOGY OF DRUG AND ALCOHOL DEPENDE
    NICHOLAS GOEDERS; Fiscal Year: 2004
    ..The primary goal of this Training Program is to provide students and young scientists with comprehensive guidance in stress and drug abuse research. ..
  52. Regulation of Pulmonary Vascular Tone During Cirrhosis
    CHRYSTELLE GARAT CARTER; Fiscal Year: 2004
    ..This project will not only define the cellular basis for hepatopulmonary syndrome, but will also contribute to our understanding of how pulmonary vascular tone is controlled at the most basic level. ..
  53. Liability Markers for Deficit Schizophrenia?
    L Hong; Fiscal Year: 2004
    ..We plan to use the preliminary data collected from this grant support to guide our full-scale search for phenotypic markers specifically associated with the liability for deficit schizophrenia and subsequent molecular genetic studies. ..
  54. Racial Segregation & Disparities in Cancer Outcomes
    Jennifer Haas; Fiscal Year: 2007
    ..The proposed study would provide empirical evidence that could give impetus to area-based interventions to reduce cancer disparities. ..
  55. ENVIRONMENTAL INFLUENCES ON COCAINE SELF-ADMINISTRATION
    NICHOLAS GOEDERS; Fiscal Year: 2007
    ..The experiments described in this revised application were designed with these stipulations in mind, taking into consideration the recommendations of the reviewers of the previous submission. ..
  56. Mast Cells: Role in the Pathophysiology of Headache
    Dan Levy; Fiscal Year: 2007
    ..Results may help identify pharmacological targets that could lead to the development of novel analgesic drugs for the treatment of headaches and possibly other intractable pain syndromes. [unreadable] [unreadable] [unreadable]..
  57. Measuring Sensitivity to Nonignorability
    Daniel Heitjan; Fiscal Year: 2003
    ..abstract_text> ..
  58. Molecular Epidemiology of Pancreatic Cancer
    Donghui Li; Fiscal Year: 2008
    ..Such information will be valuable for the primary prevention of this deadly disease. ..
  59. Mechanisms of Neurologic Disease Course
    JAMES GEDDES; Fiscal Year: 2007
    ..Dissemination of course materials will be through a course-specific web page and a multimedia CD. The course will be required for neuroscience trainees. [unreadable] [unreadable] [unreadable]..
  60. Preventing Smoking Relapse During Pregnancy and Beyond
    THOMAS BRANDON; Fiscal Year: 2006
    ..If shown to be effective, this minimal intervention would be easy and inexpensive to disseminate to women via a variety of channels and settings. ..
  61. MATERNAL HEALTH STATUS AND ADVERSE BIRTH OUTCOMES
    Jennifer Haas; Fiscal Year: 2002
    ..Such interventions should begin from the premise that improved maternal and infant outcomes can only come from improved maternal health. ..
  62. ORGANOMETALLIC SYNTHESES OF BIOACTIVE COMPOUNDS
    LOUIS HEGEDUS; Fiscal Year: 2003
    ..abstract_text> ..
  63. Treatment Issues In Smokers with Schizophrenia
    Marc Steinberg; Fiscal Year: 2008
    ..The plan will include important hands-on learning experiences, workshops, class work, attendance at national scientific conferences, and strong mentoring relationships. ..
  64. OPIOID MECHANISMS THAT FACILITATE REWARD
    KENNETH CARR; Fiscal Year: 2006
    ..abstract_text> ..
  65. Estradiol and Glutamate in the Developing Hypothalamus
    JACLYN SCHWARZ; Fiscal Year: 2007
    ..Understanding how sex effects normal brain development is necessary to understand how it may develop abnormally in psychiatric disorders. [unreadable] [unreadable] [unreadable]..
  66. MATURATION OF CEREBROVASCULAR CONTRACTILE MECHANISMS
    William Pearce; Fiscal Year: 2005
    ..abstract_text> ..
  67. MATURATION OF CEREBROVASCULAR RELAXANT MECHANISMS
    William Pearce; Fiscal Year: 2009
    ..This approach should also identify which cGMP-dependent mechanisms may be most amenable to therapeutic pharmacological manipulation in the critically ill neonate. ..
  68. CNS Mechanisms that Modulate Reward
    KENNETH CARR; Fiscal Year: 2008
    ..The research proposed in this application is aimed at elucidating midbrain and striatal mechanisms involved in the increased behavioral responsiveness of FR rats to drugs of abuse. ..