aminopyridines

Summary

Summary: Pyridines substituted in any position with an amino group. May be hydrogenated, but must retain at least one double bond.

Top Publications

  1. ncbi Roflumilast in symptomatic chronic obstructive pulmonary disease: two randomised clinical trials
    Peter M A Calverley
    School of Clinical Sciences, Liverpool, UK
    Lancet 374:685-94. 2009
  2. doi Roflumilast with long-acting β2-agonists for COPD: influence of exacerbation history
    E D Bateman
    University of Cape Town Lung Institute, Cape Town, South Africa
    Eur Respir J 38:553-60. 2011
  3. ncbi Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease
    Peter M A Calverley
    Department of Medicine, Clinical Sciences, University Hospital Aintree, Liverpool L97AL, UK
    Am J Respir Crit Care Med 176:154-61. 2007
  4. pmc A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding
    Harold B J Jefferies
    London Research Institute Cancer Research UK, Lincoln s Inn Fields Laboratories, 44 Lincoln s Inn Fields, London WC2A 3PX, UK
    EMBO Rep 9:164-70. 2008
  5. ncbi Aminopyridines correct early dysfunction and delay neurodegeneration in a mouse model of spinocerebellar ataxia type 1
    Raphael Hourez
    Laboratory of Neurophysiology, Universite Libre de Bruxelles, 1070 Brussels, Belgium
    J Neurosci 31:11795-807. 2011
  6. pmc Inhibition of the PtdIns(5) kinase PIKfyve disrupts intracellular replication of Salmonella
    Markus C Kerr
    Institute for Molecular Bioscience and ARC Centre of Excellence in Bioinformatics, The University of Queensland, St Lucia, Queensland, Australia
    EMBO J 29:1331-47. 2010
  7. ncbi Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials
    Leonardo M Fabbri
    University of Modena and Reggio Emilia, Modena, Italy
    Lancet 374:695-703. 2009
  8. pmc Transcriptional repression of the M channel subunit Kv7.2 in chronic nerve injury
    Kirstin Rose
    Institute of Membrane and Systems Biology, Faculty of Biological Science, University of Leeds, Leeds, UK
    Pain 152:742-54. 2011
  9. doi Treatment of chronic obstructive pulmonary disease with roflumilast, a new phosphodiesterase 4 inhibitor
    Nicholas J Gross
    Department of Medicine, St Francis Hospital and Medical Center, Hartford, Connecticut 06105 1208, USA
    COPD 7:141-53. 2010
  10. doi Regulation of adipocyte differentiation by activation of serotonin (5-HT) receptors 5-HT2AR and 5-HT2CR and involvement of microRNA-448-mediated repression of KLF5
    Minako Kinoshita
    Department of Cardiovascular Medicine, Graduate School of Medicine, Kyoto University, Sakyo ku, Kyoto, Japan
    Mol Endocrinol 24:1978-87. 2010

Detail Information

Publications226 found, 100 shown here

  1. ncbi Roflumilast in symptomatic chronic obstructive pulmonary disease: two randomised clinical trials
    Peter M A Calverley
    School of Clinical Sciences, Liverpool, UK
    Lancet 374:685-94. 2009
    ..We therefore investigated whether roflumilast would reduce the frequency of exacerbations requiring corticosteroids in patients with COPD...
  2. doi Roflumilast with long-acting β2-agonists for COPD: influence of exacerbation history
    E D Bateman
    University of Cape Town Lung Institute, Cape Town, South Africa
    Eur Respir J 38:553-60. 2011
    ..No differences arose in adverse events between these subgroups. Roflumilast may be used to reduce exacerbations and improve dyspnoea and lung function, without increasing adverse events in COPD patients receiving concomitant LABAs...
  3. ncbi Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease
    Peter M A Calverley
    Department of Medicine, Clinical Sciences, University Hospital Aintree, Liverpool L97AL, UK
    Am J Respir Crit Care Med 176:154-61. 2007
    ..Whether treatment is effective in more severe COPD (GOLD [Global Initiative for Chronic Obstructive Lung Disease] stages III and IV) over a longer period is unknown...
  4. pmc A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding
    Harold B J Jefferies
    London Research Institute Cancer Research UK, Lincoln s Inn Fields Laboratories, 44 Lincoln s Inn Fields, London WC2A 3PX, UK
    EMBO Rep 9:164-70. 2008
    ..We concluded that the phosphatidylinositol 3,5-bisphosphate pathway is integral to endosome formation, determining morphology and cargo flux...
  5. ncbi Aminopyridines correct early dysfunction and delay neurodegeneration in a mouse model of spinocerebellar ataxia type 1
    Raphael Hourez
    Laboratory of Neurophysiology, Universite Libre de Bruxelles, 1070 Brussels, Belgium
    J Neurosci 31:11795-807. 2011
    ..SCA1 mice are treated with aminopyridines, acting as potassium channel blockers to test whether the treatment could improve neuronal dysfunction, motor ..
  6. pmc Inhibition of the PtdIns(5) kinase PIKfyve disrupts intracellular replication of Salmonella
    Markus C Kerr
    Institute for Molecular Bioscience and ARC Centre of Excellence in Bioinformatics, The University of Queensland, St Lucia, Queensland, Australia
    EMBO J 29:1331-47. 2010
    ..Finally, although inhibition of PIKfyve in macrophages did inhibit Salmonella replication, it also appears to disrupt the macrophage's bactericidal response...
  7. ncbi Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials
    Leonardo M Fabbri
    University of Modena and Reggio Emilia, Modena, Italy
    Lancet 374:695-703. 2009
    ..The effect of roflumilast on lung function in patients with COPD that is moderate to severe who are already being treated with salmeterol or tiotropium was investigated...
  8. pmc Transcriptional repression of the M channel subunit Kv7.2 in chronic nerve injury
    Kirstin Rose
    Institute of Membrane and Systems Biology, Faculty of Biological Science, University of Leeds, Leeds, UK
    Pain 152:742-54. 2011
    ..Our work suggests a novel mechanism for neuropathic overexcitability and brings focus on M channels and REST as peripheral targets for the treatment of neuropathic pain...
  9. doi Treatment of chronic obstructive pulmonary disease with roflumilast, a new phosphodiesterase 4 inhibitor
    Nicholas J Gross
    Department of Medicine, St Francis Hospital and Medical Center, Hartford, Connecticut 06105 1208, USA
    COPD 7:141-53. 2010
    ....
  10. doi Regulation of adipocyte differentiation by activation of serotonin (5-HT) receptors 5-HT2AR and 5-HT2CR and involvement of microRNA-448-mediated repression of KLF5
    Minako Kinoshita
    Department of Cardiovascular Medicine, Graduate School of Medicine, Kyoto University, Sakyo ku, Kyoto, Japan
    Mol Endocrinol 24:1978-87. 2010
    ..In this study, we identified the regulation of adipocyte differentiation by 5-HT, 5-HT(2A)R, and 5-HT(2C)R. miR-448-mediated repression of KLF5 was identified as a negative regulator for adipocyte differentiation...
  11. pmc The reno-vascular A2B adenosine receptor protects the kidney from ischemia
    Almut Grenz
    Department of Pharmacology and Toxicology, Tubingen University Hospital, Tubingen, Germany Mucosal Inflammation Program, Department of Anesthesiology and Perioperative Medicine, University of Colorado Health Sciences Center, Denver, Colorado, USA
    PLoS Med 5:e137. 2008
    ..Here, we identified a novel pathway of renal protection from ischemia using ischemic preconditioning (IP)...
  12. pmc Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD
    Diana C Grootendorst
    Department of Pulmonology, Leiden University Medical Center, Leiden, The Netherlands
    Thorax 62:1081-7. 2007
    ..Results from in vitro studies with roflumilast indicate that it has anti-inflammatory properties that may be applicable for the treatment of COPD...
  13. doi Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial
    Jens M Hohlfeld
    Department of Clinical Airway Research, Fraunhofer Institute of Toxicology and Experimental Medicine ITEM, Nikolai Fuchs Street 1A, D 30625 Hannover, Germany
    Pulm Pharmacol Ther 21:616-23. 2008
    ..Roflumilast, an investigational, targeted phosphodiesterase 4 inhibitor, reduces the in vitro and in vivo inflammatory activity of cells such as neutrophils, eosinophils, macrophages, and monocytes...
  14. ncbi Molecular pharmacology and therapeutic potential of neuronal Kv7-modulating drugs
    Francesco Miceli
    Section of Pharmacology, Department of Neuroscience, University of Naples Federico II, Naples, Italy
    Curr Opin Pharmacol 8:65-74. 2008
    ....
  15. pmc Concomitant facilitation of GABAA receptors and KV7 channels by the non-opioid analgesic flupirtine
    Felicia Klinger
    Center for Physiology and Pharmacology, Department of Neurophysiology and Neuropharmacology, Medical University of Vienna, Austria
    Br J Pharmacol 166:1631-42. 2012
    ..It is characterized as a selective neuronal potassium channel opener (SNEPCO). Nevertheless, its mechanisms of action remain controversial and are the purpose of this study...
  16. pmc LPS-induced lung inflammation in marmoset monkeys - an acute model for anti-inflammatory drug testing
    Sophie Seehase
    Airway Research, Fraunhofer Institute for Toxicology and Experimental Medicine, Hannover, Germany
    PLoS ONE 7:e43709. 2012
    ....
  17. pmc Functional dissociation between PIKfyve-synthesized PtdIns5P and PtdIns(3,5)P2 by means of the PIKfyve inhibitor YM201636
    Diego Sbrissa
    Department of Physiology, Wayne State University School of Medicine, Detroit, Michigan, USA
    Am J Physiol Cell Physiol 303:C436-46. 2012
    ....
  18. pmc Roflumilast, a phosphodiesterase 4 inhibitor, alleviates bleomycin-induced lung injury
    J Cortijo
    Department of Pharmacology, University of Valencia, Spain
    Br J Pharmacol 156:534-44. 2009
    ..The effects of a phosphodiesterase 4 (PDE4) inhibitor, roflumilast, on bleomycin-induced lung injury were explored in 'preventive' and 'therapeutic' protocols and compared with glucocorticoids...
  19. ncbi Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily
    Gretchen M Schroeder
    Bristol Myers Squibb Research and Development, Princeton, New Jersey, 08543 4000, USA
    J Med Chem 52:1251-4. 2009
    ..Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials...
  20. ncbi Stimulation of serotonin2C receptors influences cocaine-seeking behavior in response to drug-associated stimuli in rats
    Silvia Burbassi
    Experimental Psychopharmacology, Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, 20156 Milan, Italy
    Psychopharmacology (Berl) 196:15-27. 2008
    ....
  21. ncbi The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease
    Armin Hatzelmann
    Nycomed GmbH, Konstanz, Germany
    Pulm Pharmacol Ther 23:235-56. 2010
    ..This enables roflumilast to offer effective, oral maintenance treatment for COPD, with an acceptable tolerability profile and the potential to favourably affect the extrapulmonary effects of the disease...
  22. pmc Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor
    P Malherbe
    Discovery Research CNS, F Hoffmann La Roche Ltd, Basel, Switzerland
    Br J Pharmacol 156:1326-41. 2009
    ..Herein, we describe the in vitro and in vivo properties of a selective OX(2) receptor antagonist, N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulphonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA)...
  23. ncbi Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease
    Francisco J Soto
    Division of Pulmonary and Critical Care Medicine, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
    Curr Opin Pulm Med 11:129-34. 2005
    ..Novel anti-inflammatory therapies such as selective phosphodiesterase 4 (PDE4) inhibitors are in clinical development. Their potential role in the management of COPD is described in this review...
  24. ncbi BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro
    Yao Dai
    Department of Radiation Oncology, University of Florida, Cancer Genetic Research Complex, Room 485E, Gainesville, Florida 32610, USA
    Mol Cancer Ther 9:1554-61. 2010
    ....
  25. ncbi Retigabine and flupirtine exert neuroprotective actions in organotypic hippocampal cultures
    Francesca Boscia
    Division of Pharmacology, Department of Neuroscience, School of Medicine, University of Naples Federico II, Naples, Italy
    Neuropharmacology 51:283-94. 2006
    ....
  26. doi AZD2184: a radioligand for sensitive detection of beta-amyloid deposits
    Allan E Johnson
    Disease Biology, AstraZeneca R and D, Sodertalje, Sweden
    J Neurochem 108:1177-86. 2009
    ..Taken together, the pre-clinical profile of AZD2184 in relation to the reference ligand PIB, suggests that (11)C-labeled AZD2184 is a potential radioligand for PET-visualization of beta-amyloid deposits in the living human brain...
  27. doi Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2
    Stephen Hilton
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Bioorg Med Chem 18:707-18. 2010
    ..Compounds from this series showed activity in cell-based mechanistic assays for inhibition of CHK2...
  28. pmc Effect of roflumilast on inflammatory cells in the lungs of cigarette smoke-exposed mice
    Piero A Martorana
    Department of Physiopathology and Experimental Medicine, University of Siena, Siena, Italy
    BMC Pulm Med 8:17. 2008
    ..Here we investigated the effects of roflumilast on the volume density (VV) of the inflammatory cells present in the lungs after chronic cigarette smoke exposure...
  29. ncbi M channels containing KCNQ2 subunits modulate norepinephrine, aspartate, and GABA release from hippocampal nerve terminals
    Maria Martire
    Institute of Pharmacology, School of Medicine, Catholic University of Sacred Heart, 00168 Rome, Italy
    J Neurosci 24:592-7. 2004
    ..These findings provide novel evidence for a major regulatory role of KCNQ2 K+ channel subunits in neurotransmitter release from rat hippocampal nerve endings...
  30. doi The use of aminopyridines in neurological disorders
    Saam Sedehizadeh
    Department of Clinical Neurology, Queen s Medical Centre, Nottingham, UK
    Clin Neuropharmacol 35:191-200. 2012
    b>Aminopyridines are members of a family of monoamino and diamino derivatives of pyridine, and their principal mechanism of action is dose-dependent blockade of voltage-gated potassium channels, in particular, fast voltage-gated potassium ..
  31. doi Determination of arylamines and aminopyridines in pharmaceutical products using in-situ derivatization and liquid chromatography-mass spectrometry
    Gerd Vanhoenacker
    Research Institute for Chromatography, Kortrijk, Belgium
    J Chromatogr A 1216:3563-70. 2009
    Arylamines and aminopyridines form a class of potentially genotoxic impurities (PGIs) that can be present at trace levels in active pharmaceutical ingredients (APIs)...
  32. ncbi Photoinduced amino-imino tautomerism: an infrared study of 2-amino-5-methylpyridine in a low-temperature argon matrix
    Nobuyuki Akai
    Center for Quantum Life Sciences, Hiroshima University, 1 3 1, Kagamiyama, Higashi Hiroshima, Hiroshima 739 8530, Japan
    J Phys Chem A 110:6016-22. 2006
    ..The IR spectra of 2-amino-5-methylpyridine in the T(1) state and 5-methyl-2-pyridinamino radical were also obtained by UV irradiation (lambda>or= 300 nm)...
  33. doi Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation
    Yao Dai
    Department of Radiation Oncology, University of Florida, Gainesville, FL 32610, USA
    Clin Exp Metastasis 29:253-61. 2012
    ..Together, the present findings demonstrate that the disruption of c-Met signaling by BMS-777607 significantly impairs the metastatic phenotype, suggesting that this agent may have therapeutic utility in targeting cancer metastasis...
  34. ncbi Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors
    Tobias Eckle
    Department of Anesthesiology and Intensive Care Medicine, Tubingen University Hospital, Hoppe Seyler Str 3, D 72076 Tubingen, Germany
    Circulation 115:1581-90. 2007
    ..Once generated, adenosine can activate cell-surface adenosine receptors (A1 AR, A2A AR, A2B AR, A3 AR). In the present study, we define the contribution of adenosine to cardioprotection by ischemic preconditioning...
  35. pmc Cost-effectiveness of available treatment options for patients suffering from severe COPD in the UK: a fully incremental analysis
    Nadine Hertel
    IMS Consulting Group, London, UK
    Int J Chron Obstruct Pulmon Dis 7:183-99. 2012
    ..This study aimed to assess the lifetime costs and outcomes associated with alternative treatment regimens for patients with severe COPD in the UK setting...
  36. pmc Reduction of exacerbations by the PDE4 inhibitor roflumilast--the importance of defining different subsets of patients with COPD
    Stephen I Rennard
    Nebraska Medical Center, Omaha, Nebraska, USA
    Respir Res 12:18. 2011
    ..This led to the question of whether a responsive subset existed that could be investigated further...
  37. pmc CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs
    Mike I Walton
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Sutton, United Kingdom
    Clin Cancer Res 18:5650-61. 2012
    ..We have therefore discovered a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor, CCT244747, and present its preclinical pharmacology and therapeutic activity...
  38. pmc Roflumilast attenuates allergen-induced inflammation in mild asthmatic subjects
    Gail M Gauvreau
    Department of Medicine, McMaster University, Hamilton, Ontario, Canada
    Respir Res 12:140. 2011
    ..The objective of this study was to evaluate the effects of roflumilast on bronchoconstriction, airway hyperresponsiveness (AHR), and airway inflammation in mild asthmatic patients undergoing allergen inhalation challenge...
  39. ncbi Inflammation does not precede or accompany the induction of preneoplastic lesions in the colon of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine-fed rats
    Dana Kühnel
    Nutritional Toxicology, Institute of Nutritional Science, University of Potsdam, Nuthetal, Germany
    Arch Toxicol 83:763-8. 2009
    ....
  40. pmc Symmetric double-headed aminopyridines, a novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase
    Fengtian Xue
    Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Chemistry of Life Processes Institute, Northwestern University, 2145 Sheridan Road, Evanston, Illinois 60208 3113, United States
    J Med Chem 54:2039-48. 2011
    ..These compounds provide a basis for further development of novel, potent, isoform selective, and bioavailable inhibitors for nNOS...
  41. doi Radiosynthesis of the candidate beta-amyloid radioligand [(11)C]AZD2184: Positron emission tomography examination and metabolite analysis in cynomolgus monkeys
    Jan D Andersson
    Karolinska Institutet, Department of Clinical Neuroscience, Stockholm, Sweden
    Synapse 64:733-41. 2010
    ..On the basis of the labeling chemistry and the results of the biological evaluation, we conclude that [(11)C]5 should be useful for routine clinical studies...
  42. ncbi 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential
    Yassir Younis
    Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
    J Med Chem 55:3479-87. 2012
    A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library...
  43. ncbi Roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, attenuates allergen-induced asthmatic reactions
    Emmerentia van Schalkwyk
    Department of Internal Medicine, University of Stellenbosch, Cape Town
    J Allergy Clin Immunol 116:292-8. 2005
    ..Roflumilast is an oral, once-daily inhibitor of phosphodiesterase type 4 that prevents the breakdown of cyclic adenosine monophosphate levels, leading to inhibition of proinflammatory signaling...
  44. doi Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors
    J Nicole Hamblin
    GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK
    Bioorg Med Chem Lett 18:4237-41. 2008
    ....
  45. ncbi Differential regulation of the mesoaccumbens dopamine circuit by serotonin2C receptors in the ventral tegmental area and the nucleus accumbens: an in vivo microdialysis study with cocaine
    Sylvia Navailles
    Unité Mixte de Recherche Centre National de la Recherche Scientifique UMR CNRS 5541, Universite Victor Segalen Bordeaux 2, Bordeaux Cedex, France
    Neuropsychopharmacology 33:237-46. 2008
    ....
  46. doi 5-Amino-6-chloro-N-[(1-isobutylpiperidin-4-yl)methyl]-2-methylimidazo[1,2-alpha]pyridine-8-carboxamide (CJ-033,466), a novel and selective 5-hydroxytryptamine4 receptor partial agonist: pharmacological profile in vitro and gastroprokinetic effect in consc
    Tadayoshi Mikami
    Drug Safety Research and Development, Tokyo Laboratories, Pfizer Global Research and Development, Pfizer Inc, 3 22 7 Yoyogi, Shibuya, Tokyo 151 8589, Japan
    J Pharmacol Exp Ther 325:190-9. 2008
    ..Therefore, CJ-033,466 could be used to treat gastroparesis, providing better gastroprokinetics and reduced side effects mediated by the other receptors...
  47. ncbi Differential effects of the 5-HT(2A) receptor antagonist M100907 and the 5-HT(2C) receptor antagonist SB242084 on cocaine-induced locomotor activity, cocaine self-administration and cocaine-induced reinstatement of responding
    Paul J Fletcher
    Departments of Psychiatry and Psychology, University of Toronto, Toronto, Ontario, Canada
    Neuropsychopharmacology 27:576-86. 2002
    ..These results indicate distinct, and in some cases opposite, effects of a 5-HT(2A) compared with a 5-HT(2C) receptor antagonist on various cocaine-mediated behavioral effects...
  48. pmc Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability
    M J Sanz
    Department of Pharmacology, University of Valencia, Valencia, Spain
    Br J Pharmacol 152:481-92. 2007
    ..The present study addressed the effects of the investigational PDE4 inhibitor roflumilast on leukocyte-endothelial cell interactions and endothelial permeability in vivo and in vitro...
  49. doi Effect of steady-state enoxacin on single-dose pharmacokinetics of roflumilast and roflumilast N-oxide
    Gezim Lahu
    Nycomed GmbH, Konstanz, Germany
    J Clin Pharmacol 51:586-93. 2011
    ..Roflumilast was well tolerated both alone and in combination with enoxacin. A weak interaction was shown between roflumilast and enoxacin, as mean tPDE4i increased by 25%, but is unlikely to have clinical relevance...
  50. ncbi Effect of fluvoxamine on the pharmacokinetics of roflumilast and roflumilast N-oxide
    Oliver von Richter
    Exploratory Medicine, ALTANA Pharma AG, Konstanz, Germany
    Clin Pharmacokinet 46:613-22. 2007
    ....
  51. pmc Effects of rifampicin on the pharmacokinetics of roflumilast and roflumilast N-oxide in healthy subjects
    Nassr Nassr
    Nycomed GmbH, 78467 Konstanz, Germany
    Br J Clin Pharmacol 68:580-7. 2009
    ..Roflumilast is metabolized by CYP3A4 and CYP1A2, with further involvement of CYP2C19 and extrahepatic CYP1A1. In vivo, roflumilast N-oxide contributes >90% to the total PDE4 inhibitory activity...
  52. ncbi Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke
    Piero A Martorana
    Department of Physiopathology and Experimental Medicine, University of Siena, Via Aldo Moro 6, I 53100 Siena, Italy
    Am J Respir Crit Care Med 172:848-53. 2005
    ..There is a need for new agents capable of suppressing the inflammatory response in chronic obstructive pulmonary disease...
  53. ncbi Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease
    Brian J Lipworth
    Department of Medicine and Therapeutics, Asthma and Allergy Research Group, University of Dundee, Ninewells Hospital and Medical School, Dundee DD1 9SY, UK
    Lancet 365:167-75. 2005
    ..Ultimately, clinicians will want to know whether PDE4 inhibitors are anything more than expensive "designer" theophylline, the archetypal non-selective phosphodiesterase inhibitor...
  54. ncbi [Analgesic and muscle tonus normalizing effect of flupirtine retard in chronic back pain. Results of a standardized therapeutic evaluation applying objective methods for measuring pain pressure threshold, pain pressure tolerance and muscle tension]
    G H H Müller-Schwefe
    Regionales Schmerz und Palliativzentrum DGS, Goppingen
    MMW Fortschr Med 149:153-61. 2008
    ..Flupirtine retard (Katadolon S long) has provided such an option since 2006...
  55. pmc YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes
    Ognian C Ikonomov
    Department of Physiology, Wayne State University School of Medicine, 540 E Canfield, Detroit, MI 48201, United States
    Biochem Biophys Res Commun 382:566-70. 2009
    ....
  56. ncbi Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltage independent potassium channels. Rapid communication
    J Kornhuber
    Department of Psychiatry, University of Gottingen, Federal Republic of Germany
    J Neural Transm 106:857-67. 1999
    ..This makes flupirtine the prototype of a clinically applicable substance group with analgesic, muscle-relaxant and neuroprotective properties...
  57. ncbi A phosphodiesterase 4 inhibitor, roflumilast N-oxide, inhibits human lung fibroblast functions in vitro
    F Sabatini
    Pulmonary Disease Unit, G Gaslini Institute, Largo G Gaslini 5, 16147 Genoa, Italy
    Pulm Pharmacol Ther 23:283-91. 2010
    ..Taken together, these findings indicate that roflumilast N-oxide directly targets human lung fibroblasts, which may at least partially explain the efficacy of roflumilast to mitigate a pulmonary fibrotic response in vivo...
  58. ncbi PDE4 inhibitors: a review of current developments (2005 - 2009)
    Lluís Pagès
    Almirall R and D Centre, Department of Medicinal Chemistry, Laurea Miro 408 410, 08980 Sant Feliu de Llobregat, Barcelona, Spain
    Expert Opin Ther Pat 19:1501-19. 2009
    ..Despite the sound preclinical database and some promising data from clinical trials, development of PDE4 inhibitors for the treatment of inflammatory or neurological diseases has been hampered by dose-limiting class-related side effects...
  59. ncbi Attenuation of methamphetamine induced dopaminergic neurotoxicity by flupirtine: microdialysis study on dopamine release and free radical generation
    M Gassen
    Eve Topf and National Parkinson s Foundation Centers of Excellence, Bruce Rappaport Family Research Institute, and Department of Pharmacology, Technion Faculty of Medicine, Haifa, Israel
    J Neural Transm 110:171-82. 2003
    ..This suggests that other mechanisms rather than dopamine metabolism and autoxidation, may contribute to methamphetamine neurotoxicity...
  60. pmc A clinical evaluation of amlexanox oral adhesive pellicles in the treatment of recurrent aphthous stomatitis and comparison with amlexanox oral tablets: a randomized, placebo controlled, blinded, multicenter clinical trial
    Wenxia Meng
    State Key Laboratory of Oral Diseases, West China College of Stomatology, Sichuan University, Sichuan, PR China
    Trials 10:30. 2009
    ....
  61. ncbi Phosphodiesterase type 4 inhibitors cause proinflammatory effects in vivo
    Kerryn McCluskie
    Department of Pharmacology, Theravance Inc, South San Francisco, California, USA
    J Pharmacol Exp Ther 319:468-76. 2006
    ..The proinflammatory cytokines KC and IL-8 therefore may provide surrogate biomarkers, both in preclinical animal models and in the clinic, to assess potential proinflammatory effects of this class of compounds...
  62. doi Population pharmacokinetic modelling of roflumilast and roflumilast N-oxide by total phosphodiesterase-4 inhibitory activity and development of a population pharmacodynamic-adverse event model
    Gezim Lahu
    Department of Pharmacometrics and Pharmacokinetics, Nycomed GmbH, Byk Gulden Strasse 2, Konstanz, Germany
    Clin Pharmacokinet 49:589-606. 2010
    ..Both roflumilast and its metabolite roflumilast N-oxide have anti-inflammatory properties that contribute to overall pharmacological activity...
  63. ncbi Roflumilast, a phosphodiesterase 4 inhibitor, reduces airway hyperresponsiveness after allergen challenge
    C Louw
    Internal Medicine, Lung and Allergy Unit, University of Stellenbosch, School of Medicine, Cape Town, South Africa
    Respiration 74:411-7. 2007
    ..Roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, is currently in clinical development for the treatment of asthma...
  64. ncbi S100A13 is involved in the regulation of fibroblast growth factor-1 and p40 synaptotagmin-1 release in vitro
    C Mouta Carreira
    Center for Molecular Medicine, Maine Medical Center Research Institute, South Portland, Maine 04106, USA
    J Biol Chem 273:22224-31. 1998
    ....
  65. ncbi A phosphodiesterase 4 inhibitor inhibits matrix protein deposition in airways in vitro
    Janette K Burgess
    Department of Pharmacology, University of Sydney, NSW, Australia
    J Allergy Clin Immunol 118:649-57. 2006
    ..Airway smooth muscle (ASM) cells may contribute to airway remodeling through the release of growth factors, cytokines, and extracellular matrix (ECM) proteins. The effect of current asthma therapies on this release is not known...
  66. ncbi Combination therapy with flupirtine and opioid: open-label case series in the treatment of neuropathic pain associated with cancer
    Colin S Goodchild
    Department of Anaesthesia and Perioperative Medicine, Monash University, Clayton, Victoria, Australia
    Pain Med 9:939-49. 2008
    ..This study is a case series that was designed to provide data on the efficacy and the incidence and duration of adverse effects of flupirtine in the treatment of cancer-related neuropathic pain...
  67. ncbi Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons
    Sumeer Dhar
    Department of Pediatrics, Duke University Medical Center, Durham, NC 27710, USA
    Ann Neurol 51:448-66. 2002
    ..Flupirtine may be useful as a drug capable of halting the progression of neurodegenerative diseases caused by dysregulated apoptosis...
  68. doi No dose adjustment on coadministration of the PDE4 inhibitor roflumilast with a weak CYP3A, CYP1A2, and CYP2C19 inhibitor: an investigation using cimetidine
    Gabriele M Böhmer
    Department of Clinical Pharmacology, University Hospital of Tubingen, Tubingen, Germany
    J Clin Pharmacol 51:594-602. 2011
    ..These moderate changes indicate that dose adjustment of roflumilast is not required when coadministered with a weak inhibitor of CYP1A2, CYP3A, and CYP2C19, such as cimetidine...
  69. ncbi [Use of katadolon in the treatment of abuse headache]
    M V Naprienko
    Zh Nevrol Psikhiatr Im S S Korsakova 106:38-41. 2006
    ..The period of withdrawal from drug abuse was painless. An effect of treatment remained during 1 month after the withdrawal from the drug in 11 patients, 2 patients continued to receive katadolon...
  70. ncbi Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice
    Jose Francisco Navarro
    Facultad de Psicologia, Universidad de Malaga, Spain
    Psicothema 18:100-4. 2006
    ..These findings indicate that SB-205384 exhibits an anxiolytic-like profile in the elevated plus-maze test, suggesting that GABA-A receptors which contain the alpha3 subunit might be involved in regulation of anxiety...
  71. ncbi Inhibition of inflammation and remodeling by roflumilast and dexamethasone in murine chronic asthma
    Rakesh K Kumar
    Department of Pathology, University of New South Wales, Sydney, Australia
    J Pharmacol Exp Ther 307:349-55. 2003
    ..Roflumilast did not diminish accumulation of transforming growth factor-beta1, suggesting that it might affect remodeling by mechanisms distinct from glucocorticoids...
  72. ncbi In vivo evidence that 5-HT2C receptor antagonist but not agonist modulates cocaine-induced dopamine outflow in the rat nucleus accumbens and striatum
    Sylvia Navailles
    UMR CNRS, 5541 Université Victor Segalen Bordeaux 2, Bordeaux Cedex, France
    Neuropsychopharmacology 29:319-26. 2004
    ..Furthermore, they show that 5-HT(2C) agonists, at variance with 5-HT(2C) antagonists, exert a preferential control on the impulse-stimulated release of DA...
  73. ncbi Magnesium hydroxide/aluminium hydroxide-containing antacid does not affect the pharmacokinetics of the targeted phosphodiesterase 4 inhibitor roflumilast
    Nassr Nassr
    Department of Exploratory Medicine, ALTANA Pharma AG, Byk Gulden Str 2, 78467 Konstanz, Germany
    J Clin Pharmacol 47:660-6. 2007
  74. ncbi Dose-proportional intraindividual single- and repeated-dose pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor
    Thomas D Bethke
    Department of Clinical Development Strategy, ALTANA Pharma AG, Konstanz, Germany
    J Clin Pharmacol 47:26-36. 2007
    ..Repeated oral dosing with roflumilast 250 and 500 microg once daily was well tolerated...
  75. ncbi Roflumilast, a once-daily oral phosphodiesterase 4 inhibitor, lacks relevant pharmacokinetic interactions with inhaled salbutamol when co-administered in healthy subjects
    T D Bethke
    ALTANA Pharma AG, Konstanz, Germany
    Int J Clin Pharmacol Ther 44:572-9. 2006
    ..Therefore, this study investigated the pharmacokinetic characteristics of roflumilast and its pharmacodynamically active metabolite roflumilast N-oxide when co-administered with orally inhaled salbutamol in healthy subjects...
  76. pmc Three distinct anti-allergic drugs, amlexanox, cromolyn and tranilast, bind to S100A12 and S100A13 of the S100 protein family
    T Shishibori
    Department of Chemistry, Kagawa Medical University, 1750 1, Miki cho, Kita gun, 761 0793 Kagawa, Japan
    Biochem J 338:583-9. 1999
    ..On the basis of these findings, we speculate that the three anti-allergic drugs might inhibit degranulation by binding with S100A12 and S100A13...
  77. ncbi An evaluation on the efficacy and safety of amlexanox oral adhesive tablets in the treatment of recurrent minor aphthous ulceration in a Chinese cohort: a randomized, double-blind, vehicle-controlled, unparallel multicenter clinical trial
    Jie Liu
    Department of Oral Medicine, West China College of Stomatology, Suchuan University, Sichuan, China
    Oral Surg Oral Med Oral Pathol Oral Radiol Endod 102:475-81. 2006
    ..The objectives of this study were to clinically determine the topical efficacy and safety of amlexanox oral adhesive tablets in the treatment of recurrent minor aphthous ulcerations (MiRAU) in a Chinese cohort...
  78. ncbi Investigation of a potential food effect on the pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, in healthy subjects
    Bernhard Hauns
    Department of Clinical Pharmacology, ALTANA Pharma AG, Byk Gulden Str 2, D 78467 Konstanz, Germany
    J Clin Pharmacol 46:1146-53. 2006
    ..91; 90% CI, 0.79-1.04; PE, 0.99; 90% CI, 0.92-1.06) occurred. Because roflumilast N-oxide is the major contributor to roflumilast's overall pharmacologic effects, these findings suggest that roflumilast can be taken with or without food...
  79. pmc Lack of a pharmacokinetic interaction between steady-state roflumilast and single-dose midazolam in healthy subjects
    Nassr Nassr
    ALTANA Pharma AG, 78467 Konstanz, Germany
    Br J Clin Pharmacol 63:365-70. 2007
    ..The aim of this study was to investigate the effects of roflumilast, an investigational PDE4 inhibitor for the treatment of COPD and asthma, on the pharmacokinetics of the CYP3A probe drug midazolam and its major metabolites...
  80. ncbi Steady-state pharmacokinetics of roflumilast and roflumilast N-oxide in patients with mild and moderate liver cirrhosis
    Robert Hermann
    Exploratory Medicine, ALTANA Pharma AG, Konstanz, Germany
    Clin Pharmacokinet 46:403-16. 2007
    ..Roflumilast is being developed for the treatment of inflammatory airway diseases such as chronic obstructive pulmonary disease and asthma...
  81. ncbi Effect of inhaled roflumilast on the prevention and resolution of allergen-induced late phase airflow obstruction in Brown Norway rats
    Richard W Chapman
    Schering Plough Research Institute, Pulmonary and Peripheral Neurobiology M S 1700, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States
    Eur J Pharmacol 571:215-21. 2007
    ..These results support the development of inhaled PDE4 inhibitors for the treatment of asthma and COPD, particularly for the improvement of lung function...
  82. pmc Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion
    Atsushi Kuno
    Department of Physiology, MSB 3074, University of South Alabama, College of Medicine, Mobile, AL 36688, USA
    J Mol Cell Cardiol 43:262-71. 2007
    ..We propose that the key protective event in IPC occurs when PKC increases the heart's sensitivity to adenosine so that endogenous adenosine can activate A(2b)-dependent signaling...
  83. ncbi The oral, once-daily phosphodiesterase 4 inhibitor roflumilast lacks relevant pharmacokinetic interactions with inhaled budesonide
    Robert Hermann
    ALTANA Pharma AG, Konstanz, Germany
    J Clin Pharmacol 47:1005-13. 2007
    ..67, 1.50). Coadministration of roflumilast and budesonide did not alter the steady-state disposition of each other and did not affect safety and tolerability of either drug...
  84. ncbi Metal-free catalysts for the hydrolysis of RNA derived from guanidines, 2-aminopyridines, and 2-aminobenzimidazoles
    Ute Scheffer
    Institute for Organic Chemistry and Chemical Biology, Goethe University Frankfurt, Marie Curie Str 11, 60439 Frankfurt am Main, Germany
    J Am Chem Soc 127:2211-7. 2005
    ..Conjugates of 10b with antisense oligonucleotides or RNA binding peptides, therefore, will be promising candidates as site specific artificial ribonucleases...
  85. ncbi In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor
    D S Bundschuh
    Department of Pharmacology, Byk Gulden, P O Box 10 03 10, 78403 Konstanz, Germany
    J Pharmacol Exp Ther 297:280-90. 2001
    ..These results, coupled with the in vitro effects of roflumilast on inflammatory cells, suggest that roflumilast represents a potential new drug for the treatment of asthma and chronic obstructive pulmonary disease...
  86. ncbi Phosphodiesterase 4 inhibitors for the treatment of COPD
    Graham Sturton
    Bayer plc, Pharma Research, Stoke Court, Stoke Poges, Slough SL2 4LY, Berkshire, UK
    Chest 121:192S-196S. 2002
    ..The initial clinical data on the most advanced compound, cilomilast, were indeed encouraging. However, full knowledge of the therapeutic value of this novel compound class awaits the outcome of longer term clinical trials...
  87. ncbi Effect of repeated dose of erythromycin on the pharmacokinetics of roflumilast and roflumilast N-oxide
    G Lahu
    Nycomed GmbH formerly ALTANA Pharma AG, Konstanz, Germany
    Int J Clin Pharmacol Ther 47:236-45. 2009
    ..Both roflumilast and roflumilast N-oxide have similar intrinsic PDE4 inhibitory activity; the total PDE4 inhibition (tPDE4i) in humans is likely due to the combined effect of roflumilast and roflumilast N-oxide...
  88. doi The targeted oral, once-daily phosphodiesterase 4 inhibitor roflumilast and the leukotriene receptor antagonist montelukast do not exhibit significant pharmacokinetic interactions
    Gabriele M Böhmer
    Department of Clinical Pharmacology, University Hospital of Tubingen, Otfried Müller Str 45, D 72076 Tubingen, Germany
    J Clin Pharmacol 49:389-97. 2009
    ..Concomitant administration of both drugs was well tolerated. These findings suggest that no dose adjustment is warranted for either drug when roflumilast and montelukast are coadministered...
  89. doi PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts
    Shinsaku Togo
    Pulmonary and Critical Care Medicine, University of Nebraska Medical Center, Omaha, NE 68198 5885, USA
    Am J Physiol Lung Cell Mol Physiol 296:L959-69. 2009
    ..The present study supports the concept that PDE4 inhibitors may attenuate fibroblast activities that can lead to fibrosis and that PDE4 inhibitors may be particularly effective in the presence of TGF-beta1-induced fibroblast stimulation...
  90. doi Effect of single and repeated doses of ketoconazole on the pharmacokinetics of roflumilast and roflumilast N-oxide
    Gezim Lahu
    Nycomed GmbH, Department of Pharmacometrics and Pharmacokinetics, Byk Gulden Str 2, 78467 Konstanz, Germany
    J Clin Pharmacol 48:1339-49. 2008
    ..No clinically relevant adverse events were observed. Coadministration of ketoconazole and roflumilast does not require dose adjustment of roflumilast...
  91. ncbi The new phosphodiesterase 4 inhibitor roflumilast is efficacious in exercise-induced asthma and leads to suppression of LPS-stimulated TNF-alpha ex vivo
    Wolfgang Timmer
    Byk Gulden Pharmaceuticals, Konstanz, Germany
    J Clin Pharmacol 42:297-303. 2002
    ..It is concluded that roflumilast is effective in the treatment of exercise-induced asthma. This result was accompanied by a significant reduction of TNF-alpha levels ex vivo. Treatment with roflumilast was safe and well tolerated...
  92. doi Single-dose pharmacokinetics of roflumilast in children and adolescents
    Kathleen A Neville
    Department of Pediatrics, University of Missouri Kansas City and the Children s Mercy Hospitals and Clinics, 2401 Gillham Road, Kansas City, MO 64079, USA
    J Clin Pharmacol 48:978-85. 2008
    ..1 and 0.8 microg/L per 1 microg/kg dose for adolescents and children, respectively), pharmacokinetic parameters for roflumilast and roflumilast N-oxide were not different between age groups and were similar to adults...
  93. ncbi Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors
    L Wollin
    ALTANA Pharma, Byk Gulden Strasse 2, 78467 Konstanz, Germany
    Pulm Pharmacol Ther 19:343-52. 2006
    ..This study suggests that roflumilast has anti-inflammatory action and provides rationale for the investigation of roflumilast in asthmatic patients...
  94. pmc PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast
    Victoria Boswell-Smith
    The Sackler Institute of Pulmonary Pharmacology, King s College London School of Biomedical and Health Sciences, King s College London, Guys Campus, UK
    Int J Chron Obstruct Pulmon Dis 2:121-9. 2007
    ..This review will discuss the current standing of PDE4 inhibitors like roflumilast as novel treatments for COPD and the potential for developing nonemetic anti-inflammatory drugs...
  95. ncbi Effectiveness of two oral pastes for the treatment of recurrent aphthous stomatitis
    M Rodriguez
    Facultad de Odontologia, Universidad Nacional de Colombia, Bogota, Colombia
    Oral Dis 13:490-4. 2007
    ..To compare the effectiveness of two topical medications to reduce the pain and size of recurrent minor aphthous ulcers...
  96. ncbi Treatment strategies for recurrent oral aphthous ulcers
    R W Barrons
    Clinical Pharmacy, Xavier University of Louisiana, 1 Drexel Street, New Orleans, LA 70125 1098, USA
    Am J Health Syst Pharm 58:41-50; quiz 51-3. 2001
    ..Thalidomide is effective but, because of its toxicity and cost, should be used only as an alternative to oral corticosteroids. RAU can be effectively managed with a variety of topical and systemic medications...
  97. ncbi Roflumilast inhibits lipopolysaccharide-induced inflammatory mediators via suppression of nuclear factor-kappaB, p38 mitogen-activated protein kinase, and c-Jun NH2-terminal kinase activation
    Hyun Jeong Kwak
    Laboratory of Molecular Pharmacology and Physiology, Medicinal Science Division, Korea Research Institute of Chemical Technology, P O Box 107, Yusung Gu, TaeJon 305 343, Korea
    J Pharmacol Exp Ther 315:1188-95. 2005
    ..These results suggest that the inhibitory activity of roflumilast on the production of inflammatory mediators seems to be mediated via inhibition of NF-kappaB, p38 MAP kinase, and JNK activation in macrophages...
  98. ncbi Roflumilast inhibition of pulmonary leukotriene production and bronchoconstriction in ovalbumin-sensitized and -challenged Guinea pigs
    Lutz Wollin
    ALTANA Pharma, Konstanz, Germany
    J Asthma 42:873-8. 2005
    ..06 mg/kg) and LTB4 (ID50 = 0.05 mg/kg) release versus placebo-treated animals. Roflumilast did not affect LTD4-induced bronchoconstriction. These findings support the role of roflumilast as an anti-inflammatory treatment for asthma...
  99. ncbi The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro
    N A Jones
    Sackler Institute of Pulmonary Pharmacology, 5th Floor Hodgkin Building, Guy s Campus, St Thomas School of Biomedical Sciences, King s College, London SE1 1UL, UK
    Pulm Pharmacol Ther 18:93-101. 2005
    ..These data provide further evidence that selective PDE4 isoenzyme inhibitors can inhibit neutrophil degranulation, effects not shared by PDE3 inhibitors or theophylline...
  100. ncbi Roflumilast--an oral anti-inflammatory treatment for chronic obstructive pulmonary disease: a randomised controlled trial
    Klaus F Rabe
    Leiden University Medical Centre, Leiden, Netherlands
    Lancet 366:563-71. 2005
    ..There are few treatment options for the disease. This study assessed the efficacy and safety of roflumilast, a phosphodiesterase-4 inhibitor, in patients with moderate to severe COPD...
  101. ncbi A comparative study of the efficacy of Aphtheal in the management of recurrent minor aphthous ulceration
    Brenda Murray
    The Oral Science Research Centre, School of Dentistry, Queen s University Belfast, UK
    J Oral Pathol Med 34:413-9. 2005
    ..Recurrent minor aphthous ulceration (RAU) is a common condition which is multifactorial in origin...

Research Grants108 found, 100 shown here

  1. Principles of Therapy in Cerebellar Disease: Explorations in Ion Channel Mutants
    John Stahl; Fiscal Year: 2009
    ..Results of these experiments will allow us to test published speculations that aminopyridines exert their beneficial effects by restoring normal Purkinje cell activity...
  2. CHEMISTRY SUPPORT SERVICES TO THE ENVIRONMENTAL TOXICOLOGY PROGRAM
    STEVE GRAVES; Fiscal Year: 2009
    ..A collection Alkylanilines were procured and purity determined in support of in vitro studies. Aminopyridines to be used in a 90-day gavage study were analyzed for purity...
  3. CHEMISTRY SUPPORT SERVICES TO THE ENVIRONMENTAL TOXICOLOGY PROGRAM
    STEVE GRAVES; Fiscal Year: 2010
    ..Purity analysis for a planned aminopyridines subchronic gavage study is complete...
  4. STRUCTURE-FUNCTION IN LOW-RESISTANCE JUNCTIONS
    Camillo Peracchia; Fiscal Year: 1993
    ..by testing their potential interaction with amphiphilic connexin domains and the effects of xanthines and aminopyridines. The nature of extracellular connexin-connexin interactions will be studied by expressing connexins ..
  5. PROPERTIES OF THE INWARD RECTIFIER OF SKELETAL MUSCLE
    PAUL HOROWICZ; Fiscal Year: 1980
    ..e., Barium, quaternary ammonium ions, aminopyridines) will be also studied...
  6. CELLULAR NEUROPHARMACOLOGICAL STUDY OF DRUG ACTION
    Toshio Narahashi; Fiscal Year: 1980
    ..The studies of grayanotoxins, deoxycholate and pancuronium and aminopyridines are among such examples...
  7. TAS::75 0862::TAS - NTP TOXICOLOGIC POTENTIAL OF SELECTED TEST AGENTS
    LU TAYLOR; Fiscal Year: 2011
    Studies to evaluate Aminopyridines by Gavage in F344/NTac Rats and B6C3F1 Mice
  8. Stressor controllability and anxiety: role of serotonin and prefrontal cortex.
    John Christianson; Fiscal Year: 2008
    ..The proposed research will provide critical insight to how the key psychological variable of coping contributes to the development or prevention of anxiety/PTSD after a traumatic event...
  9. NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITY
    OSMOND D CRUZ; Fiscal Year: 2001
    ..The preclinical data on in vivo efficacies of WHI-05 and WHI-07 will be essential to further explore the utility of these novel drugs for clinical studies in human patients. ..
  10. NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITY
    OSMOND D CRUZ; Fiscal Year: 2000
    ..The preclinical data on in vivo efficacies of WHI-05 and WHI-07 will be essential to further explore the utility of these novel drugs for clinical studies in human patients. ..
  11. Transmitter Repletion: Key to Phrenic-Diaphragm Function
    Erik van Lunteren; Fiscal Year: 2005
    ..These studies may lead to novel therapeutic approaches to respiratory muscle impairment and resulting hypercapnic respiratory failure for conditions which produce neuromuscular junction dysfunction. ..
  12. Phase II SBIR: WHI-07: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ....
  13. Vanadocenes as a New Class of Spermicidal Drugs
    OSMOND D CRUZ; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  14. METVAN: A Novel Anticancer Agent
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The knowledge gained from these studies described under Specific Aims 1-2 is expected to facilitate the design of innovative treatment regimens employing METVAN for metastatic breast cancer and brain tumor patients. ..
  15. Transmitter Repletion: Key to Phrenic-Diaphragm Function
    Erik van Lunteren; Fiscal Year: 2002
    ..These studies may lead to novel therapeutic approaches to respiratory muscle impairment and resulting hypercapnic respiratory failure for conditions which produce neuromuscular junction dysfunction. ..
  16. Transmitter Repletion: Key to Phrenic-Diaphragm Function
    Erik van Lunteren; Fiscal Year: 2003
    ..These studies may lead to novel therapeutic approaches to respiratory muscle impairment and resulting hypercapnic respiratory failure for conditions which produce neuromuscular junction dysfunction. ..
  17. PHI 346: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..Following successful completion of the Phase I in vivo efficacy studies, gel formulation of PHI-346 will be further explored as a vaginal dual-function microbicide in Phase II. ..
  18. FLP-102: Rationally Engineered Antiviral Protein
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The preclinical data on FLP-102 will be essential to further explore the utility of this novel recombinant PAP mutant for Phase II. ..
  19. Viral-induced Adaptation of Neutrophil Response in ARDS
    JERRY NICK; Fiscal Year: 2007
    ..End of Abstract) ..
  20. PHI-443: Novel Non-Spermicidal Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..Specific Aims 1 and 2 may provide the foundation for the clinical development of PHI-443 in Phase II studies as a safe, effective broad-spectrum anti-HIV microbicide without conception-inhibiting functions. ..
  21. NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITY
    OSMOND D CRUZ; Fiscal Year: 1999
    ..The preclinical data on in vivo efficacies of WHI-05 and WHI-07 will be essential to further explore the utility of these novel drugs for clinical studies in human patients. ..
  22. Viral-induced Adaptation of Neutrophil Response in ARDS
    JERRY NICK; Fiscal Year: 2008
    ..End of Abstract) ..
  23. Transmitter Repletion: Key to Phrenic-Diaphragm Function
    Erik van Lunteren; Fiscal Year: 2004
    ..These studies may lead to novel therapeutic approaches to respiratory muscle impairment and resulting hypercapnic respiratory failure for conditions which produce neuromuscular junction dysfunction. ..
  24. Stampidine: A Novel Broad-Spectrum Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ..Specific Aims 1 and 2 may provide the foundation for the clinical development of STAMP in Phase II studies as a safe, effective broad-spectrum anti-HIV microbicide without conception-inhibiting functions. ..
  25. BFGF LOW AFFINITY RECEPTORS AND HIVAN
    Patricio Ray; Fiscal Year: 2006
    ..These studies will demonstrate that growth factors release into the circulation of HIV- infected children can accelerate the progression of HIVAN, and test new therapies against this disease. [unreadable] [unreadable]..
  26. Pathogenesis of HIV-Associated HUS in Children
    Patricio Ray; Fiscal Year: 2006
    ..abstract_text> ..
  27. Pathogenesis of HIV-HUS in children
    PATRICIO ERNESTO RAY; Fiscal Year: 2010
    ....
  28. BFGF LOW AFFINITY RECEPTORS AND HIVAN
    Patricio Ray; Fiscal Year: 2002
    ..All these studies will provide new knowledge that could be applied clinically to develop new treatments to prevent the progression of HIVAN in children. ..
  29. Molecular Epidemiology, Virulence, and Genomic Characterization of Ureaplasmas
    Ken Waites; Fiscal Year: 2007
    ....
  30. Neural Mechanism of Drug-Seeking Behavior
    Janet Neisewander; Fiscal Year: 2009
    ..Understanding these circuits will likely have important implications for developing treatments for cocaine dependence. ..
  31. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2004
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  32. A Thermo Electron LTQ Mass Spectrometer
    Joseph Zaia; Fiscal Year: 2006
    ..The salary for the instrument operator will be provided by the Dean of BU School of Medicine. [unreadable] [unreadable]..
  33. Effects of Chronic THC in Adolescence
    Peter J Winsauer; Fiscal Year: 2010
    ..Together, data from these experiments will demonstrate how drug abuse and hormonal status during adolescence may permanently alter brain function and the liability of subsequent abuse of A9-THC. ..
  34. Neural Mechanism of Drug-Seeking Behavior
    Janet L Neisewander; Fiscal Year: 2010
    ..Understanding these circuits will likely have important implications for developing treatments for cocaine dependence. ..
  35. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2002
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  36. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2006
    ..This will eventually lead to a better understanding of abuse prevention and treatment modalities. ..
  37. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2004
    ..This will eventually lead to a better understanding of abuse prevention and treatment modalities. ..
  38. Drugs as conditioned reinforcers and/or enhancers of social reward in adolescents
    Janet Neisewander; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  39. CB1 Modulation of Opioid Peptides and Ethanol Intake
    Loren Parsons; Fiscal Year: 2006
    ..abstract_text> ..
  40. 5-HTIB RECEPTORS AND MECHANISMS OF ETHANOL REINFORCEMENT
    Loren Parsons; Fiscal Year: 2005
    ..abstract_text> ..
  41. CB1 Modulation of Opioid Peptides and Ethanol Intake
    Loren Parsons; Fiscal Year: 2004
    ..abstract_text> ..
  42. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2003
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  43. INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMA
    KIAN CHUNG; Fiscal Year: 2004
    ..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
  44. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2007
    ..This will eventually lead to a better understanding of abuse prevention and treatment modalities. ..
  45. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 2004
    ..abstract_text> ..
  46. Limbic-cortical involvement in drug seeking
    Janet Neisewander; Fiscal Year: 2004
    ..The findings may be useful for developing behavioral and pharmacological treatments for cocaine dependence. ..
  47. CB1 Modulation of Opioid Peptides and Ethanol Intake
    Loren Parsons; Fiscal Year: 2007
    ..abstract_text> ..
  48. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2003
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  49. SELECTIVE SEROTONERGIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2003
    ..Radioligand binding and functional assays will be conducted. The 5-HT1F ligand is not selective; we propose to explore its structure-activity relationships and functional activity in an attempt to develop a 5-HT1F-selective ligand. ..
  50. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 1990
    ..A long-term objective of the proposed research is to achieve an understanding of these complex behavioral effects in biochemical terms and thus to facilitate rational clinical intervention...
  51. SELECTIVE SEROTONERGIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2001
    ..Radioligand binding and functional assays will be conducted. The 5-HT1F ligand is not selective; we propose to explore its structure-activity relationships and functional activity in an attempt to develop a 5-HT1F-selective ligand. ..
  52. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 1999
    ..It is proposed to further investigate each of these concepts by synthesizing (where necessary) and evaluating the appropriate agents. ..
  53. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 1999
    ..If confirmed, the findings would suggest a new pharmacologic treatment strategy for cocaine dependence. ..
  54. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 1992
    ..New agents are proposed for synthesis that will aid in solving these problems...
  55. CHEMICAL/BEHAVIORAL STUDIES ON HALLUCINOGENIC AGENTS
    RICHARD GLENNON; Fiscal Year: 1993
    ..New agents are proposed for synthesis that will aid in solving these problems...
  56. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 2001
    ..abstract_text> ..
  57. SELECTIVE SEROTONERGIC AGENTS
    RICHARD GLENNON; Fiscal Year: 2002
    ..Radioligand binding and functional assays will be conducted. The 5-HT1F ligand is not selective; we propose to explore its structure-activity relationships and functional activity in an attempt to develop a 5-HT1F-selective ligand. ..
  58. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 2003
    ..abstract_text> ..
  59. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 2002
    ..abstract_text> ..
  60. Limbic-cortical involvement in drug seeking
    Janet Neisewander; Fiscal Year: 2006
    ..The findings may be useful for developing behavioral and pharmacological treatments for cocaine dependence. ..
  61. Neural Mechanism of Drug-Seeking Behavior
    Janet L Neisewander; Fiscal Year: 2010
    ..Understanding these circuits will likely have important implications for developing treatments for cocaine dependence. ..
  62. Behavioral and Pharmacological Analysis of Drugs of Abuse
    JERROLD WINTER; Fiscal Year: 2008
    ..This likelihood coupled with continued interest in the therapeutic use of agents such as psilocybin makes a detailed pharmacological assessment of these drugs of utmost importance. ..
  63. Neural Mechanism of Drug-Seeking Behavior
    Janet Neisewander; Fiscal Year: 2007
    ..Understanding these circuits will likely have important implications for developing treatments for cocaine dependence. ..
  64. BEHAVIORAL AND PHARMACOLOGIC ANALYSIS OF DRUG OF ABUSE
    JERROLD WINTER; Fiscal Year: 1999
    ....
  65. INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMA
    KIAN CHUNG; Fiscal Year: 2003
    ..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
  66. Drugs as conditioned reinforcers and/or enhancers of social reward in adolescents
    Janet Neisewander; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  67. Neural Mechanism of Drug-Seeking Behavior
    Janet Neisewander; Fiscal Year: 2008
    ..Understanding these circuits will likely have important implications for developing treatments for cocaine dependence. ..
  68. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 1991
    ..A long-term objective of the proposed research is to achieve an understanding of these complex behavioral effects in biochemical terms and thus to facilitate rational clinical intervention...
  69. Limbic-cortical involvement in drug seeking
    Janet Neisewander; Fiscal Year: 2003
    ..The findings may be useful for developing behavioral and pharmacological treatments for cocaine dependence. ..
  70. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2001
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  71. INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMA
    KIAN CHUNG; Fiscal Year: 2001
    ..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
  72. CNS VIRAL INJURY AND VULNERABILITY TO OPIATE DRUG ABUSE
    Marylou Solbrig; Fiscal Year: 2002
    ..At the conclusion of the grant period, the requisite skills in behavioral pharmacology, neuropharmacology and molecular biology for continued work in the study and treatment of drug addiction will have been acquired by the candidate. ..
  73. Viral neuropathology neuropeptides and epilepsy
    Marylou Solbrig; Fiscal Year: 2004
    ....
  74. INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMA
    KIAN CHUNG; Fiscal Year: 2002
    ..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
  75. Limbic-cortical involvement in drug seeking
    Janet Neisewander; Fiscal Year: 2002
    ..The findings may be useful for developing behavioral and pharmacological treatments for cocaine dependence. ..
  76. Limbic-cortical involvement in drug seeking
    Janet Neisewander; Fiscal Year: 2003
    ..The findings may be useful for developing behavioral and pharmacological treatments for cocaine dependence. ..
  77. EFFECTS OF DIOXINS (TCDD) ON CARDIAC ION CHANNELS
    Desuo Wang; Fiscal Year: 2003
    ....
  78. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2000
    ..If confirmed, the findings would suggest a new pharmacologic treatment strategy for cocaine dependence. ..
  79. Viral neuropathology neuropeptides and epilepsy
    Marylou Solbrig; Fiscal Year: 2005
    ....
  80. BEHAVIORAL AND PHARMACOLOGIC ANALYSIS OF DRUG OF ABUSE
    JERROLD WINTER; Fiscal Year: 2000
    ....
  81. NEURAL MECHANISMS OF DRUG SEEKING BEHAVIOR
    Janet Neisewander; Fiscal Year: 2002
    ..These experiments will help to elucidate 5-HT mechanisms involved in incentive motivation for cocaine and will likely have important implications for developing treatments for cocaine dependence. ..
  82. AMBIENT PARTICULATE MATTERS POISON CARDIAC ION CHANNELS
    Desuo Wang; Fiscal Year: 2005
    ....
  83. INFLAMMATION & CORTICOSTEROID RESPONSES IN SEVERE ASTHMA
    KIAN CHUNG; Fiscal Year: 2005
    ..The molecular mechanisms underlying loss of CR will be examined. These studies should lead to more effective therapies for chronic severe asthma. ..
  84. BEHAVIORAL & PHARMACOLOGICAL ANALYSIS OF DRUGS OF ABUSE
    JERROLD WINTER; Fiscal Year: 2005
    ..abstract_text> ..