benzazepines

Summary

Summary: Compounds with BENZENE fused to AZEPINES.

Top Publications

  1. pmc Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channels
    A Bucchi
    Laboratory of Molecular Physiology and Neurobiology, Department of Biomolecular Sciences and Biotechnology, University of Milano, Italy
    J Physiol 572:335-46. 2006
  2. ncbi Ivabradine and outcomes in chronic heart failure (SHIFT): a randomised placebo-controlled study
    Karl Swedberg
    Department of Emergency and Cardiovascular Medicine, Sahlgrenska Academy, University of Gothenburg, Goteborg, Sweden
    Lancet 376:875-85. 2010
  3. ncbi Heart rate as a prognostic risk factor in patients with coronary artery disease and left-ventricular systolic dysfunction (BEAUTIFUL): a subgroup analysis of a randomised controlled trial
    Kim Fox
    Royal Brompton Hospital, London, UK
    Lancet 372:817-21. 2008
  4. 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
  5. 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
  6. pmc Chronic heart rate reduction by ivabradine prevents endothelial dysfunction in dyslipidaemic mice
    A Drouin
    Montreal Heart Institute, Research Center, Faculty of Medicine, Department of Surgery, Universite de Montreal, Montreal, Quebec, Canada
    Br J Pharmacol 154:749-57. 2008
  7. 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
  8. 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
  9. 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
  10. ncbi Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina
    Jean Claude Tardif
    Montreal Heart Institute, 5000 Belanger Street, Montreal, Quebec H1T 1C8, Canada
    Eur Heart J 26:2529-36. 2005

Research Grants

  1. CELLULAR DOPAMINE RECEPTOR COINCIDENCE
    MARJORIE ARIANO; Fiscal Year: 1993
  2. High Dose Nicotine Patch Therapy for Spit Tobacco Users
    Jon Ebbert; Fiscal Year: 2004
  3. Brief Dental Office Intervention with Tobacco Quitline
    Jon Ebbert; Fiscal Year: 2005
  4. Evaluating Nicotine Lozenges for Treatment of Smokeless Tobacco Addiction
    Jon Ebbert; Fiscal Year: 2009
  5. CNS Mechanisms that Modulate Reward
    KENNETH CARR; Fiscal Year: 2008
  6. AASK Cohort Study
    Kenneth Jamerson; Fiscal Year: 2008
  7. OPIOID MECHANISMS THAT FACILITATE REWARD
    KENNETH CARR; Fiscal Year: 2006
  8. Gradual vs Abrupt Cessation Treatment for Smoking
    John Hughes; Fiscal Year: 2007
  9. Lateral Hypothalamus, Dopamine and Ingestive Behavior
    David Wirtshafter; Fiscal Year: 2007
  10. EVALUATION OF A CIGARETTE SUBSTITUTE
    John Hughes; Fiscal Year: 2001

Detail Information

Publications310 found, 100 shown here

  1. pmc Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channels
    A Bucchi
    Laboratory of Molecular Physiology and Neurobiology, Department of Biomolecular Sciences and Biotechnology, University of Milano, Italy
    J Physiol 572:335-46. 2006
    ..The mode of action of ivabradine on the two channels is discussed by implementing a simplified version of a previously developed model of f-channel kinetics...
  2. ncbi Ivabradine and outcomes in chronic heart failure (SHIFT): a randomised placebo-controlled study
    Karl Swedberg
    Department of Emergency and Cardiovascular Medicine, Sahlgrenska Academy, University of Gothenburg, Goteborg, Sweden
    Lancet 376:875-85. 2010
    ..Raised resting heart rate is a risk factor for adverse outcomes. We aimed to assess the effect of heart-rate reduction by the selective sinus-node inhibitor ivabradine on outcomes in heart failure...
  3. ncbi Heart rate as a prognostic risk factor in patients with coronary artery disease and left-ventricular systolic dysfunction (BEAUTIFUL): a subgroup analysis of a randomised controlled trial
    Kim Fox
    Royal Brompton Hospital, London, UK
    Lancet 372:817-21. 2008
    ..We did a subanalysis of this placebo group to test the hypothesis that elevated resting heart rate at baseline is a marker for subsequent cardiovascular death and morbidity...
  4. 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...
  5. 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...
  6. pmc Chronic heart rate reduction by ivabradine prevents endothelial dysfunction in dyslipidaemic mice
    A Drouin
    Montreal Heart Institute, Research Center, Faculty of Medicine, Department of Surgery, Universite de Montreal, Montreal, Quebec, Canada
    Br J Pharmacol 154:749-57. 2008
    ..We tested the hypothesis that a reduction of resting heart rate with the cardiac pacemaker I(f) current inhibitor ivabradine prevents the endothelial dysfunction associated with dyslipidaemia...
  7. 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...
  8. 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...
  9. 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...
  10. ncbi Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina
    Jean Claude Tardif
    Montreal Heart Institute, 5000 Belanger Street, Montreal, Quebec H1T 1C8, Canada
    Eur Heart J 26:2529-36. 2005
    ..Ivabradine has shown anti-ischaemic and anti-anginal activity in a placebo-controlled trial. The objective of this study was to compare the anti-anginal and anti-ischaemic effects of ivabradine and the beta-blocker atenolol...
  11. ncbi A single intravenous dose of ivabradine, a novel I(f) inhibitor, lowers heart rate but does not depress left ventricular function in patients with left ventricular dysfunction
    Matthias Manz
    Department of Cardiology, Marienhof Hospital, Koblenz, Germany
    Cardiology 100:149-55. 2003
    ..Thus, a single intravenous dose of ivabradine produced a substantial reduction in resting heart rate without affecting LV function in patients with regional or global LV dysfunction...
  12. ncbi Effects on outcomes of heart rate reduction by ivabradine in patients with congestive heart failure: is there an influence of beta-blocker dose?: findings from the SHIFT (Systolic Heart failure treatment with the I(f) inhibitor ivabradine Trial) study
    Karl Swedberg
    Department of Emergency and Cardiovascular Medicine, Sahlgrenska Academy, University of Gothenburg, Goteborg, Sweden
    J Am Coll Cardiol 59:1938-45. 2012
    ..This study used the SHIFT (Systolic Heart failure treatment with the I(f) inhibitor ivabradine Trial) database to assess the impact of background beta-blocker dose on response to ivabradine...
  13. 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...
  14. 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...
  15. ncbi Heart rate as a risk factor in chronic heart failure (SHIFT): the association between heart rate and outcomes in a randomised placebo-controlled trial
    Michael Bohm
    Universitatsklinikum des Saarlandes, Klinik fur Innere Medizin III, Homburg Saar, Germany
    Lancet 376:886-94. 2010
    ..We aimed to test our hypothesis by investigating the association between heart rate and events in this patient population...
  16. ncbi Heart rate lowering by specific and selective I(f) current inhibition with ivabradine: a new therapeutic perspective in cardiovascular disease
    Dario DiFrancesco
    Dipartimento di Scienze Biomolecolari e Biotecnologie, Universita di Milano, Milan, Italy
    Drugs 64:1757-65. 2004
    ..Experimental data indicate a potential role of pure heart rate lowering in other cardiovascular conditions, such as heart failure...
  17. ncbi Ivabradine for patients with stable coronary artery disease and left-ventricular systolic dysfunction (BEAUTIFUL): a randomised, double-blind, placebo-controlled trial
    Kim Fox
    Royal Brompton Hospital, London, UK
    Lancet 372:807-16. 2008
    ..We aimed to test whether lowering the heart rate with ivabradine reduces cardiovascular death and morbidity in patients with coronary artery disease and left-ventricular systolic dysfunction...
  18. 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...
  19. ncbi Dopamine increases the gain of the input-output response of rat prefrontal pyramidal neurons
    Kay Thurley
    Department of Physiology, University of Bern, Buehlplatz 5, CH 3012 Bern, Switzerland
    J Neurophysiol 99:2985-97. 2008
    ..The results support the hypothesis that catecholamines increase the neuronal gain and suggest that dopamine improves working memory via gain modulation...
  20. ncbi I(f) inhibition in cardiovascular diseases
    Catherine Thollon
    Cardiovascular Department, Institut de Recherches Servier, Suresnes, France
    Adv Pharmacol 59:53-92. 2010
    ....
  21. ncbi MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo
    Jessica J Huck
    Millennium Pharmaceuticals, Cambridge, MA 02139, USA
    Mol Cancer Res 8:373-84. 2010
    ..Taken together, this data shows that senescence is a terminal outcome of Aurora A inhibition and supports the evaluation of senescence biomarkers in clinic samples...
  22. ncbi Heart rate reduction during exercise-induced myocardial ischaemia and stunning
    Xavier Monnet
    Laboratoire de Pharmacologie, INSERM E 00 01, Faculte de Medecine Paris Sud, Paris, France
    Eur Heart J 25:579-86. 2004
    ..The effects of selective heart rate reduction by ivabradine (If inhibitor) were compared to those of atenolol on exercise-induced ischaemia and stunning...
  23. ncbi Contributions of heart rate and contractility to myocardial oxygen balance during exercise
    Patrice Colin
    Laboratoire de Pharmacologie, INSERM E 00 01, Faculte de Medecine Paris Sud, 94270 Le Kremlin Bicetre, France
    Am J Physiol Heart Circ Physiol 284:H676-82. 2003
    ..Thus HR reduction and negative inotropy equally contribute to the reduction in MVo(2) during exercise in the normal heart. The negative inotropy limits the increase in DT afforded by HR reduction...
  24. ncbi Heart rate reduction by ivabradine reduces oxidative stress, improves endothelial function, and prevents atherosclerosis in apolipoprotein E-deficient mice
    Florian Custodis
    Klinik fur Innere Medizin III, Kardiologie, Angiologie und Internistische Intensivmedizin, Universitatsklinikum des Saarlandes, 66424 Homburg Saar, Germany
    Circulation 117:2377-87. 2008
    ..We hypothesized that selective heart rate reduction may influence endothelial function and atherogenesis and tested the effects of the I(f) current inhibitor ivabradine in apolipoprotein E-deficient mice...
  25. ncbi Mesocortical dopamine neurons operate in distinct temporal domains using multimodal signaling
    Antonieta Lavin
    Department of Physiology and Neuroscience, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Neurosci 25:5013-23. 2005
    ....
  26. ncbi Activation of the intracellular renin-angiotensin system in cardiac fibroblasts by high glucose: role in extracellular matrix production
    Vivek P Singh
    Cardiovascular Research Institute, Texas A and M HSC, Temple, TX 76504, USA
    Am J Physiol Heart Circ Physiol 294:H1675-84. 2008
    ....
  27. ncbi Ivabradine induces an increase in ventricular fibrillation threshold during acute myocardial ischemia: an experimental study
    Fanny Vaillant
    Laboratory of Medical Pharmacology, INSERM ERI 22, Grange Blanche Medical School, Claude Bernard University, Lyon, France
    J Cardiovasc Pharmacol 52:548-54. 2008
    ..Tachycardia often facilitates ischemic ventricular fibrillation (VF)...
  28. ncbi Effect of Carvedilol, Ivabradine or their combination on exercise capacity in patients with Heart Failure (the CARVIVA HF trial)
    Maurizio Volterrani
    Department of Medical Sciences, IRCCS San Raffaele Roma, Rome, Italy
    Int J Cardiol 151:218-24. 2011
    ..We performed a randomised open blinded endpoint study to assess the effect of heart rate reduction with carvedilol, ivabradine, and their combination on exercise capacity in HF patients receiving maximal dose of ACE inhibitor...
  29. ncbi Ivabradine in combination with beta-blocker improves symptoms and quality of life in patients with stable angina pectoris: results from the ADDITIONS study
    Karl Werdan
    Department of Medicine III, University Hospital Halle Saale of the Martin Luther University Halle Wittenberg, Halle Saale, Germany
    Clin Res Cardiol 101:365-73. 2012
    ....
  30. ncbi Dopamine is involved in food-anticipatory activity in mice
    Yuan Yuan Liu
    Department of Pharmacology, Shanghai Medical College, Fudan University, Shanghai, China
    J Biol Rhythms 27:398-409. 2012
    ..These results strongly indicate that the dopaminergic system plays an essential role in the FAA in mice...
  31. pmc Effects of selective heart rate reduction with ivabradine on left ventricular remodelling and function: results from the SHIFT echocardiography substudy
    Jean Claude Tardif
    Montreal Heart Institute, Universite de Montreal, 5000 Belanger Street, Montreal, Quebec, Canada H1T 1C8
    Eur Heart J 32:2507-15. 2011
    ..The SHIFT echocardiographic substudy evaluated the effects of ivabradine on left ventricular (LV) remodelling in heart failure (HF)...
  32. ncbi Heart rate reduction with ivabradine and health related quality of life in patients with chronic heart failure: results from the SHIFT study
    Inger Ekman
    Institute of Health and Care Sciences, Sahlgrenska Academy, Box 457, SE 405 30 Gothenburg, Sweden
    Eur Heart J 32:2395-404. 2011
    ..The aim was to evaluate whether heart rate (HR) reduction with ivabradine can translate into increased HQoL in parallel to a reduction of primary outcomes in SHIFT...
  33. 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...
  34. 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...
  35. 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...
  36. ncbi Highly cytotoxic copper(II) complexes with modified paullone ligands
    Michael F Primik
    Institute of Inorganic Chemistry, University of Vienna, Austria
    Inorg Chem 49:302-11. 2010
    ..All of the compounds evaluated are cytotoxic, with complexes 3 and 4 exhibiting IC(50) values in the nanomolar range...
  37. 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...
  38. pmc Dopamine D1 vs D5 receptor-dependent induction of seizures in relation to DARPP-32, ERK1/2 and GluR1-AMPA signalling
    Gerard J O'Sullivan
    Molecular and Cellular Therapeutics and RCSI Research Institute, Royal College of Surgeons in Ireland, Dublin 2, Ireland
    Neuropharmacology 54:1051-61. 2008
    ..These findings indicate that D(1), and to a lesser extent D(5), receptor coupling to DARPP-32, ERK1/2 and glutamatergic signalling is involved in mediating the convulsant effects of SKF 83822...
  39. 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...
  40. ncbi Relationship between ivabradine treatment and cardiovascular outcomes in patients with stable coronary artery disease and left ventricular systolic dysfunction with limiting angina: a subgroup analysis of the randomized, controlled BEAUTIFUL trial
    Kim Fox
    Royal Brompton Hospital, Sydney Street, London, UK
    Eur Heart J 30:2337-45. 2009
    ..We performed a post hoc analysis of the effect of ivabradine in BEAUTIFUL patients whose limiting symptom at baseline was angina, particularly in terms of coronary outcomes...
  41. ncbi Dopamine and memory: modulation of the persistence of memory for novel hippocampal NMDA receptor-dependent paired associates
    Ingrid Bethus
    Laboratory for Cognitive Neuroscience, Centre for Cognitive and Neural Systems, The University of Edinburgh, Edinburgh EH8 9JZ, United Kingdom
    J Neurosci 30:1610-8. 2010
    ....
  42. ncbi Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women
    Steven R Smith
    Pennington Biomedical Research Center, Louisiana State University System, Baton Rouge, Louisiana, USA
    Obesity (Silver Spring) 17:494-503. 2009
    ..Lorcaserin was well tolerated and efficacious for weight reduction in this 12-week study. Longer-term trials employing behavior modification will be needed to more fully assess its safety and efficacy...
  43. pmc Methamphetamine induces dopamine D1 receptor-dependent endoplasmic reticulum stress-related molecular events in the rat striatum
    Subramaniam Jayanthi
    Molecular Neuropsychiatry Research Branch, National Institute of Drug Abuse, National Institutes of Health NIH Department of Health and Human Services DHHS, Intramural Research Program, Baltimore, MD, USA
    PLoS ONE 4:e6092. 2009
    ..Our data also suggest that METH-induced toxicity might be a useful model to dissect molecular mechanisms involved in ER stress-dependent events in the rodent brain...
  44. ncbi Psychiatric adverse events in randomized, double-blind, placebo-controlled clinical trials of varenicline: a pooled analysis
    Serena Tonstad
    Department of Preventive Cardiology, Oslo University Hospital Ulleval, Oslo, Norway
    Drug Saf 33:289-301. 2010
    ..In postmarketing surveillance, neuropsychiatric symptoms have appeared; however, their incidence and causal relationship to varenicline is not known...
  45. pmc Efficacy of the I(f) current inhibitor ivabradine in patients with chronic stable angina receiving beta-blocker therapy: a 4-month, randomized, placebo-controlled trial
    Jean Claude Tardif
    Montreal Heart Institute, Universite de Montreal, Montreal, Quebec, Canada
    Eur Heart J 30:540-8. 2009
    ..To evaluate the anti-anginal and anti-ischaemic efficacy of the selective I(f) current inhibitor ivabradine in patients with chronic stable angina pectoris receiving beta-blocker therapy...
  46. ncbi Synergistic requirements for the induction of dopaminergic D1/D5-receptor-mediated LTP in hippocampal slices of rat CA1 in vitro
    Sheeja Navakkode
    Leibniz Institute for Neurobiology, Department of Neurophysiology, Magdeburg, Germany
    Neuropharmacology 52:1547-54. 2007
    ..e. NMDA-receptor activation. We provide first evidence that a synergistic role of D1/D5- as well as NMDA-receptor-function is required in mediating processes relevant for the maintenance of this protein synthesis-dependent potentiation...
  47. ncbi Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties
    Leopoldo Luistro
    Discovery Oncology, Discovery Chemistry, In Silico Sciences, Non Clinical Safety, Drug Metabolism, and RNA Therapeutics, Hoffmann La Roche, Inc, Nutley, New Jersey, USA
    Cancer Res 69:7672-80. 2009
    ..These preclinical results support evaluation of RO4929097 in clinical studies using an intermittent dosing schedule. A multicenter phase I dose escalation study in oncology is under way...
  48. 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...
  49. ncbi Antagonizing dopamine D1-like receptor inhibits Th17 cell differentiation: preventive and therapeutic effects on experimental autoimmune encephalomyelitis
    Kazuhisa Nakano
    The Department of Allergy and Immunology, Faculty of Medicine, Saitama Medical University, 38 Morohongo, Moroyama, Saitama 350 0495, Japan
    Biochem Biophys Res Commun 373:286-91. 2008
    ..Adoptive transfer of DCs treated with SCH23390 successfully prevented EAE. These findings indicate that antagonizing D1-like-Rs on DCs inhibits Th17 differentiation, thereby leading to an amelioration of EAE...
  50. ncbi Antianginal efficacy and safety of ivabradine compared with amlodipine in patients with stable effort angina pectoris: a 3-month randomised, double-blind, multicentre, noninferiority trial
    Witold Ruzyllo
    Department of Coronary Artery Disease and Cardiac Catheterization Laboratory, Institute of Cardiology, Warsaw, Poland
    Drugs 67:393-405. 2007
    ..This study was undertaken to compare the antianginal and anti-ischaemic effects of the novel heart-rate-lowering agent ivabradine and of the calcium channel antagonist amlodipine...
  51. ncbi Dopamine modulates excitability of basolateral amygdala neurons in vitro
    Sven Kroner
    Center for Neural Basics Cognition, Deptartment of Neuroscience, University of Pittsburgh, Pittsburgh, Penssylvania
    J Neurophysiol 93:1598-610. 2005
    ....
  52. ncbi Long-term heart rate reduction induced by the selective I(f) current inhibitor ivabradine improves left ventricular function and intrinsic myocardial structure in congestive heart failure
    Paul Mulder
    INSERM U644, UFR de Medecine et de Pharmacie, Rouen, France
    Circulation 109:1674-9. 2004
    ..However, the long-term effects of HRR on cardiac function and remodeling are unknown...
  53. ncbi Dopaminergic modulation of motor maps in rat motor cortex: an in vivo study
    J A Hosp
    Clinical Neurorehabilitation, Department of Neurology, University of Zurich, Frauenklinikstr 26, 8091 Zurich, Switzerland
    Neuroscience 159:692-700. 2009
    ..By enhancing intracortical excitability and signal transduction, D2-mediated dopaminergic signaling may affect movement execution, e.g. by enabling task-related muscle activation synergies, and learning...
  54. pmc Use-dependent inhibition of hHCN4 by ivabradine and relationship with reduction in pacemaker activity
    C Thollon
    Division Pathologies Cardiaques et Vasculaires, Institut de Recherches Servier, 11 rue des Moulineaux, Suresnes 92150, France
    Br J Pharmacol 150:37-46. 2007
    ....
  55. ncbi Heart rate reduction with ivabradine improves energy metabolism and mechanical function of isolated ischaemic rabbit heart
    Claudio Ceconi
    Department of Cardiology, University of Ferrara, Corso Giovecca, 203, 44100 Ferrara, Italy
    Cardiovasc Res 84:72-82. 2009
    ..We report an ex vivo study to evaluate the anti-ischaemic effect of ivabradine in terms of modulation of cardiac energy metabolism...
  56. 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...
  57. ncbi Chronic heart rate reduction remodels ion channel transcripts in the mouse sinoatrial node but not in the ventricle
    Anne Laure Leoni
    Institut National de la Sante et de la Recherche Medicale INSERM, U533, l institut du thorax, Nantes, France
    Physiol Genomics 24:4-12. 2005
    ..We conclude that reducing HR induces a complex remodeling of ion channel expression in the SAN but has little impact on ion channel transcripts in the ventricle...
  58. pmc Aurora kinase A inhibition leads to p73-dependent apoptosis in p53-deficient cancer cells
    Altaf A Dar
    Departments of Surgery, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA
    Cancer Res 68:8998-9004. 2008
    ..Taken together, our results indicate that AURKA regulates TAp73-dependent apoptosis and highlight the potential of the AURKA inhibitor MLN8054 in treating cancers that are defective in p53 signaling...
  59. ncbi Heart rate reduction with ivabradine increases ischaemia-induced ventricular fibrillation threshold: role of myocyte structure and myocardial perfusion
    Fanny Vaillant
    INSERM ERI22, Université Claude Bernard de Lyon, 8 avenue Rockefeller, 69373 Lyon Cedex 08, France
    Resuscitation 82:1092-9. 2011
    ..This study investigated myocyte ultrastructure and regional myocardial blood flow (RMBF), potentially involved in these cardioprotective effects of IVA...
  60. ncbi Power fluctuations in beta and gamma frequencies in rat globus pallidus: association with specific phases of slow oscillations and differential modulation by dopamine D1 and D2 receptors
    Cyril Dejean
    Department of Anatomy and Structural Biology, School of Medical Sciences, University of Otago, Dunedin 9054, New Zealand
    J Neurosci 31:6098-107. 2011
    ..Disruption of this hierarchical organization and subsequent disordered beta-gamma balance in basal ganglia disorders such as Parkinson's disease may be important in the pathogenesis of their symptoms...
  61. pmc Methamphetamine and dopamine receptor D1 regulate entrainment of murine circadian oscillators
    Jennifer A Mohawk
    Department of Biology, University of Virginia, Charlottesville, Virginia, United States of America
    PLoS ONE 8:e62463. 2013
    ..This study also identifies a role for dopamine signaling in normal entrainment of circadian oscillators...
  62. ncbi Innovation in coronary artery disease and heart failure: clinical benefits of pure heart rate reduction with ivabradine
    Emmanuel Canet
    Institut de Recherches Internationales Servier, Courbevoie, France
    Ann N Y Acad Sci 1222:90-9. 2011
    ..The development of ivabradine represents a clear innovation in the management of cardiovascular disease...
  63. ncbi Safety of ivabradine in patients with coronary artery disease and left ventricular systolic dysfunction (from the BEAUTIFUL Holter Substudy)
    Michal Tendera
    Medical University of Silesia, Katowice, Poland
    Am J Cardiol 107:805-11. 2011
    ..Our observations strongly support the safety of combining ivabradine with β blockers in patients with coronary artery disease...
  64. 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...
  65. ncbi Heart rate reduction by ivabradine reduces diastolic dysfunction and cardiac fibrosis
    David Busseuil
    Research Center, Montreal Heart Institute, Universite de Montreal, Montreal, Quebec, Canada
    Cardiology 117:234-42. 2010
    ..To determine if heart rate (HR) reduction with ivabradine (IVA), a selective inhibitor of the pacemaker I(f) current, prevents cardiac dysfunction associated with dyslipidemia...
  66. ncbi Efficacy of ivabradine in combination with Beta-blocker versus uptitration of Beta-blocker in patients with stable angina
    E Amosova
    National Medical University, Kiev, Ukraine
    Cardiovasc Drugs Ther 25:531-7. 2011
    ..This pilot study compared the antianginal and anti-ischemic efficacy and hemodynamic profile of ivabradine plus 5 mg bisoprolol versus those of 10 mg bisoprolol in patients with stable angina...
  67. ncbi Ivabradine improves coronary flow reserve in patients with stable coronary artery disease
    Emmanouil I Skalidis
    Cardiology Department, University Hospital of Heraklion, and Biostatistics Lab, University of Crete, Crete, Greece
    Atherosclerosis 215:160-5. 2011
    ..The purpose of this study was to assess the effects of ivabradine on coronary flow velocity and flow reserve (CFR) in patients with stable coronary artery disease (CAD)...
  68. 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
    ....
  69. ncbi Heart rate at baseline influences the effect of ivabradine on cardiovascular outcomes in chronic heart failure: analysis from the SHIFT study
    Michael Bohm
    Klinik fur Innere Medizin III, Kardiologie, Angiologie und Internistische Intensivmedizin, Universitatsklinikum des Saarlandes, Kirrberger Str 1, 66424, Homburg Saar, Germany
    Clin Res Cardiol 102:11-22. 2013
    ..A cut-off value of ≥75 bpm was chosen by the EMEA for approval for the use of ivabradine in chronic heart failure...
  70. pmc Implications of plasma protein binding for pharmacokinetics and pharmacodynamics of the γ-secretase inhibitor RO4929097
    Jianmei Wu
    Karmanos Cancer Institute, Wayne State University, Detroit, MI 48201, USA
    Clin Cancer Res 18:2066-79. 2012
    ..This study investigated RO4929097 binding in plasma and its implications for the pharmacokinetics and pharmacodynamics of this compound...
  71. 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...
  72. ncbi Impact of ''off-label'' use of ivabradine on exercise capacity, gas exchange, functional class, quality of life, and neurohormonal modulation in patients with ischemic chronic heart failure
    Filippo M Sarullo
    Division of Cardiology, Buccheri La Ferla Fatebenefratelli Hospital, Palermo, Italy
    J Cardiovasc Pharmacol Ther 15:349-55. 2010
    ..The purpose of this study was to evaluate the impact of ''Off-Label'' use of ivabradine on exercise capacity, gas exchange, functional class, quality of life, and neurohormonal modulation in pts with ischemic CHF...
  73. ncbi D2-dopamine receptor blockade impairs motion detection in goldfish
    C Mora-Ferrer
    Institut für Zoologie III J Gutenberg Universität, Mainz, Germany
    Vis Neurosci 17:177-86. 2000
    ..The effect of sulpiride is discussed in relation to known sulpiride effects on retinal neurons and the retinal pigment epithelium...
  74. 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...
  75. 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...
  76. 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...
  77. 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...
  78. ncbi The discovery of the selective I(f) current inhibitor ivabradine. A new therapeutic approach to ischemic heart disease
    J P Vilaine
    Institut de Recherches Servier, Division Pathologies Cardiaques et Vasculaires, 11 rue des Moulineaux, 92150 Suresnes, France
    Pharmacol Res 53:424-34. 2006
    ....
  79. 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...
  80. ncbi Opposing roles of D1 and D2 receptors in appetitive conditioning
    Yaniv S Eyny
    Department of Psychology and Program in Neurobiology and Behavior, Columbia University, New York, New York 10027, USA
    J Neurosci 23:1584-7. 2003
    ....
  81. ncbi Specific inhibition of HCN channels slows rhythm differently in atria, ventricle and outflow tract and stabilizes conduction in the anoxic-reoxygenated embryonic heart model
    Alexandre Sarre
    Department of Physiology, Faculty of Biology and Medicine, 7 rue du Bugnon, CH 1005 Lausanne, Switzerland
    Pharmacol Res 61:85-91. 2010
    ..Thus, HCN channels are specifically distributed and control finely atrial, ventricular and outflow tract pacemakers as well as conduction in the embryonic heart under normoxia and throughout anoxia-reoxygenation...
  82. pmc Partial agonists of the α3β4* neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in rats
    Susmita Chatterjee
    Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA 94608, USA
    Neuropsychopharmacology 36:603-15. 2011
    ..CP-601932 has been shown to be safe in humans and may represent a potential novel treatment for AUDs...
  83. pmc Organometallic indolo[3,2-c]quinolines versus indolo[3,2-d]benzazepines: synthesis, structural and spectroscopic characterization, and biological efficacy
    Lukas K Filak
    Institute of Inorganic Chemistry, University of Vienna, Wahringer Strasse 42, 1090, Vienna, Austria
    J Biol Inorg Chem 15:903-18. 2010
    ..L ( 1 )) and N'-(11H-indolo[3,2-c]quinolin-6-yl)-N,N-dimethylethane-1,2-diamine (L ( 2 )) and indolo[3,2-d]benzazepines N-(7,12-dihydroindolo-[3,2-d][1]benzazepin-6-yl)-ethane-1,2-diamine (L ( 3 )) and N'-(7,12-dihydroindolo-[3,2-d]..
  84. ncbi Preservation of coronary reserve by ivabradine-induced reduction in heart rate in infarcted rats is associated with decrease in perivascular collagen
    Eduard I Dedkov
    Department of Biomedical Sciences, New York College of Osteopathic Medicine NYIT, Old Westbury, NY 11568, USA
    Am J Physiol Heart Circ Physiol 293:H590-8. 2007
    ..Therefore, our data reveal that improved maximal myocardial perfusion and coronary reserve in MI + IVA rats are most likely the result of reduced periarteriolar collagen rather than enhanced arteriolar growth...
  85. pmc Stopping smokeless tobacco with varenicline: randomised double blind placebo controlled trial
    Karl Fagerström
    Smokers Information Centre, Fagerstrom Consulting AB, Berga Alle 1, 25452 Helsingborg, Sweden
    BMJ 341:c6549. 2010
    ..To assess the efficacy and safety of varenicline (a licensed cigarette smoking cessation aid) in helping users of smokeless tobacco to quit...
  86. ncbi Heart rate reduction with ivabradine prevents the global phenotype of left ventricular remodeling
    Claudio Ceconi
    Department of Cardiology, University of Ferrara, Ferrara, Italy
    Am J Physiol Heart Circ Physiol 300:H366-73. 2011
    ..05). The HR-reducing properties of ivabradine prevent changes in the global phenotype of LV remodeling in the rat, optimize energy consumption, and avoid electrophysiological and structural remodeling...
  87. ncbi Metal-based paullones as putative CDK inhibitors for antitumor chemotherapy
    Wolfgang F Schmid
    Institute of Inorganic Chemistry, University of Vienna, Wahringerstr 42, A 1090 Vienna, Austria
    J Med Chem 50:6343-55. 2007
    ..3)H-Thymidine incorporation assays revealed the compounds to lower the rate of DNA synthesis, and flow cytometric analyses showed cell cycle arrest mainly in G 0/ G 1 phase...
  88. 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...
  89. pmc Pleiotropic action(s) of the bradycardic agent ivabradine: cardiovascular protection beyond heart rate reduction
    G Heusch
    Institute for Pathophysiology, University of Essen Medical School, Essen, Germany
    Br J Pharmacol 155:970-1. 2008
    ..The heart rate dependency of ivabradine's benefit for atherosclerotic vascular function is contradictory, and that on post-infarct remodelling is entirely unclear...
  90. ncbi Multicenter, placebo-controlled trial of lorcaserin for weight management
    Steven R Smith
    Translational Research Institute for Metabolism and Diabetes, Florida Hospital and the Sanford Burnham Institute, Winter Park, FL 32789, USA
    N Engl J Med 363:245-56. 2010
    ..Lorcaserin is a selective serotonin 2C receptor agonist that could be useful in reducing body weight...
  91. 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...
  92. 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...
  93. ncbi 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta
    Conrad Kunick
    Institut fur Pharmazeutische Chemie, Technische Universitat Braunschweig, Beethovenstrasse 55, 38106, Braunschweig, Germany
    Bioorg Med Chem Lett 14:413-6. 2004
    ..The charge distribution within the 1-azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-azakenpaullone compared to other paullone derivatives...
  94. ncbi Activation of phosphatidylinositol-linked D1-like receptor modulates FGF-2 expression in astrocytes via IP3-dependent Ca2+ signaling
    Xinhua Zhang
    Laboratory of Molecular Cell Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China
    J Neurosci 29:7766-75. 2009
    ..PI-linked D(1)-like receptor plays an important role in the regulation of astrocytic FGF-2 expression and neuroprotection which may provide a potential target for the drug discovery in Parkinson's disease...
  95. ncbi Evidence for the sensitivity of operant timing behaviour to stimulation of D1 dopamine receptors
    T H C Cheung
    Psychopharmacology Section, Division of Psychiatry, University of Nottingham, Room B109, Medical School, Queen s Medical Centre, Nottingham, NG7 2UH, UK
    Psychopharmacology (Berl) 195:213-22. 2007
    ..It is not known whether this effect of d-amphetamine is mimicked by direct D(1)-like receptor stimulation...
  96. ncbi Therapeutic potential of vasopressin receptor antagonists
    Farhan Ali
    Heart Failure Program, Wayne State University, Detroit, Michigan, USA
    Drugs 67:847-58. 2007
    ..Ongoing clinical trials should further define the scope of the potential therapeutic role of VRAs...
  97. ncbi Heterosynaptic co-activation of glutamatergic and dopaminergic afferents is required to induce persistent long-term potentiation
    Colin M O'Carroll
    Department of Neuroscience, 1, George Square, University of Edinburgh, Edinburgh EH8 9JZ, UK
    Neuropharmacology 47:324-32. 2004
    ....
  98. pmc Cocaine-predictive stimulus induces drug-seeking behavior and neural activation in limbic brain regions after multiple months of abstinence: reversal by D(1) antagonists
    R Ciccocioppo
    Department of Neuropharmacology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Proc Natl Acad Sci U S A 98:1976-81. 2001
    ..Moreover, the results implicate D(1)-dependent neural mechanisms within the medial prefrontal cortex and basolateral amygdala as substrates for cocaine-seeking behavior elicited by cocaine-predictive environmental stimuli...
  99. 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...
  100. 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
    ....
  101. ncbi Improvement of regional myocardial blood flow and function and reduction of infarct size with ivabradine: protection beyond heart rate reduction
    Gerd Heusch
    Institut fur Pathophysiologie, Universitatsklinikum Essen, Essen, Germany
    Eur Heart J 29:2265-75. 2008
    ..Heart rate reduction by beta-blockade is associated with negative inotropism and unmasked alpha-adrenergic coronary vasoconstriction. Ivabradine is the only available bradycardic agent for clinical use...

Research Grants66

  1. CELLULAR DOPAMINE RECEPTOR COINCIDENCE
    MARJORIE ARIANO; Fiscal Year: 1993
    ..D1 receptors stimulate adenylyl cyclase and bind substituted benzazepines; D2 receptors inhibit cyclic AMP formation and are inhibited by neuroleptic drugs...
  2. 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. ..
  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. 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. ..
  5. 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. ..
  6. AASK Cohort Study
    Kenneth Jamerson; Fiscal Year: 2008
    ..Ultimately, data from the AASK Cohort Study should enhance our understanding of the determine the progression of kidney disease. Such results might eventually lead to new ESRD. ..
  7. OPIOID MECHANISMS THAT FACILITATE REWARD
    KENNETH CARR; Fiscal Year: 2006
    ..abstract_text> ..
  8. 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. ..
  9. Lateral Hypothalamus, Dopamine and Ingestive Behavior
    David Wirtshafter; Fiscal Year: 2007
    ..Gaining an understanding of these systems is a prerequisite for the rational development of novel treatments for disturbances of ingestion, such as occur in obesity, bulemia and cahchexia. [unreadable] [unreadable] [unreadable]..
  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. 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. ..
  12. A Simple Measure for Studying Sensory Gating Deficits
    Neal Swerdlow; Fiscal Year: 2007
    ..abstract_text> ..
  13. NEURAL CIRCUITRY OF SENSORIMOTOR GATING ACROSS SPECIES
    Neal Swerdlow; Fiscal Year: 2006
    ....
  14. 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. ..
  15. 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. ..
  16. Consequences of repeated kappa receptor activation on brain stimulation reward
    Elena Chartoff; Fiscal Year: 2006
    ..abstract_text> ..
  17. Neuroscience at the Boundaries of Neurology and Psychiatry
    Neal Swerdlow; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  18. GEORGETOWN UNIVERSITY-MEDSTAR CENTER FOR CLINICAL AND TRANSLATIONAL SCIENCE
    Joseph Verbalis; Fiscal Year: 2006
    ..The planning process will be led by a committee of faculty members who are leaders in translational research and clinical research training at the member institutions. [unreadable] [unreadable] [unreadable]..
  19. Role of dopamine D1 receptors in morphine withdrawal
    Elena Chartoff; Fiscal Year: 2006
    ..This work may lead to new pharmacotherapies that can alleviate aversive and dysphoric states associated with opiate withdrawal and perhaps reduce relapse to drug taking. ..
  20. SEX DIFFERENCES IN NICOTINE REINFORCEMENT: HUMAN/ANIMAL
    Kenneth Perkins; Fiscal Year: 2003
    ....
  21. 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. ..
  22. MOTOR ACTIONS OF CANNABINOIDS IN A PARKINSONS MODEL
    CLARA SANUDO PENA; Fiscal Year: 2002
    ..Behavioral, biochemical, and physiological studies will be conducted in parallel to test this possibility. It will also help integrate the cannabinergic system with the current knowledge of basal ganglia physiology. ..
  23. BRAIN OXYTOCIN AND ETHANOL EFFECT ON INGESTIVE BEHAVIOR
    Joseph Verbalis; Fiscal Year: 2001
    ....
  24. DISCRIMINATIVE STIMULUS EFFECTS OF NICOTINE
    Kenneth Perkins; Fiscal Year: 2001
    ....
  25. Neural basis of heritable DA-mediated gating deficits
    Neal R Swerdlow; Fiscal Year: 2010
    ....
  26. Natural History of Attempts to Stop Smoking
    John R Hughes; Fiscal Year: 2010
    ....
  27. PHYSIOLOGICAL ADAPTATION TO SUSTAINED HYPO-OSMOLALITY
    Joseph Verbalis; Fiscal Year: 2002
    ..These studies should lead to an elucidation of the cellular mechanisms underlying one of the most basic and intriguing unanswered question about clinically hyponatremic disorders. ..
  28. BASAL GANGLIA CIRCUITRY IMMEDIATE EARLY GENE EXPRESSION
    David Wirtshafter; Fiscal Year: 2003
    ..Other studies will examine the effects of lesions within the basal ganglia on the IEG expression induced by systemic administration of dopaminergic drugs. ..
  29. HYPONATREMIA-INDUCED OSTEOPOROSIS
    Joseph G Verbalis; Fiscal Year: 2010
    ....
  30. CORTICO-STRIATAL SUBSTRATES OF DEFICIENT STARTLE GATING
    Neal R Swerdlow; Fiscal Year: 2010
    ..New information from these studies will be a foundation for innovative models of the pathophysiology of schizophrenia and other inherited neuropsychiatric disorders, and for prospective strategies for novel drug development. ..
  31. OPIOID DEPRESSION OF RESPIRATORY NEURONS
    PETER LALLEY; Fiscal Year: 2003
    ..It will also test a new method that may alleviate opioid-induced depression of respiration without affecting analgesia, and counteract respiratory depression by overdose of opioids. ..
  32. 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. ..
  33. Dopamine mechanisms in development of type-2 diabetes
    Andras Hajnal; Fiscal Year: 2008
    ..These studies will help determine how plasticity in the dopaminergic system affects behavioral and metabolic factors related to hyperphagia and the development of dietary-induced NIDDM. ..
  34. 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. ..
  35. Nicotine Intake in Smokers with Schizophrenia
    Jill Williams; Fiscal Year: 2009
    ....
  36. 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. ..
  37. Simulated Human Pharmacokinetics in Rat: Methylphenidate
    Ronald Kuczenski; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  38. Northeast Under/Grad Research Organization for Neuroscience
    Cheryl Frye; Fiscal Year: 2008
    ..Both of these outcomes are congruous with the Public Health Service's mission to ensure that there is a resource of well-trained scientists and health-care providers in the United States. [unreadable] [unreadable] [unreadable]..
  39. 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. ..
  40. ASK, ADVISE, REFER: Promoting Pharmacy-based Referrals to Tobacco Quitlines
    Karen S Hudmon; Fiscal Year: 2010
    ....
  41. Structural Studies of AIDS-Responsive Drugs
    Vivian Cody; Fiscal Year: 2010
    ..These results will help guide the design of species selective inhibitors. Mutagenesis studies will be carried out to test these possibilitiesin the structure-based correlations to help design novel pjDHFRinhibitors. ..
  42. Treatment of Nicotine Dependence in Health Care Setting
    Gary Swan; Fiscal Year: 2009
    ....
  43. 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. ..
  44. 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...
  45. DOPAMINE TRANSMISSION IN ALCOHOLISM
    Anissa Abi Dargham; Fiscal Year: 2002
    ..Understanding the neurochemical abnormalities underlying vulnerability to alcoholism would guide future treatment interventions and risk prevention strategies. ..
  46. 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. ..
  47. 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. ..
  48. GUSTATORY REWARD AND DOPAMINE IN THE NUCLEUS ACCUMBENS
    Andras Hajnal; Fiscal Year: 2003
    ..This knowledge is directly relevant to understanding the control of normal ingestive behavior and to the maladies related to this essential behavior, such as obesity, anorexia nervosa, bulimia nervosa, and binge eating disorder. ..
  49. MECHANISM OF ACTION OF DRUGS OF ABUSE--AMPHETAMINE
    Ronald Kuczenski; Fiscal Year: 2004
    ..The possibility of nonsynaptic release sites on nigrostriatal DA afferents will be assessed by labeling components of the release mechanism and then correlating them with the locations of dopamine receptors. ..
  50. COCAINE SELF ADMINISTRATION IN DOPAMINE KNOCKOUT MICE
    SIMON CAINE; Fiscal Year: 2003
    ..abstract_text> ..
  51. PASSIVE IMMUNITY TO COCAINE USING NOVEL HUMAN ANTIBODIES
    Andrew Norman; Fiscal Year: 2003
    ..These studies will form the basis for an application to the FDA for advancement of an identified human monoclonal anti-cocaine antibody to Phase II clinical trials to determine the efficacy of a passive immunotherapy of cocaine abuse. ..
  52. 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. ..
  53. PET Imaging of Serotonin Transmission in MDMA Users
    Anissa Abi Dargham; Fiscal Year: 2008
    ..abstract_text> ..
  54. 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]..
  55. PREFRONTAL D1 AND 5HT1A RECEPTORS IN SCHIZOPHRENIA
    Anissa Abi Dargham; Fiscal Year: 2001
    ..This study will lead to a better understanding of neurochemical abnormalities in schizophrenia, their relations to symptomatology, and their implications for treatment. ..
  56. 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. ..
  57. 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. ..
  58. Prefrontal cortical dopamine and cognition-schizophrenia
    Anissa Abi Dargham; Fiscal Year: 2007
    ..abstract_text> ..
  59. Angiotensin II Mediates Early Changes in Diabetic Kidney
    Helmy Siragy; Fiscal Year: 2007
    ..The proposed studies will help understand the mechanisms that are involved in diabetic the development of new therapeutic modalities to prevent or slowdown the development ..
  60. CVD RISK FACTORS AND BRAIN MORPHOLOGY IN NHLBI TWINS
    Gary Swan; Fiscal Year: 2001
    ....
  61. 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]..
  62. 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. ..
  63. 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. ..
  64. African American Study of Kidney Disease and Hypertensi*
    Robert Toto; Fiscal Year: 2007
    ..Such results might eventually lead to new strategies that delay or prevent ESRD. ..
  65. 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. ..