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