nicotinic agonists

Summary

Summary: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.

Top Publications

  1. ncbi Immunomodulatory effects of cigarette smoke
    M L Sopori
    Pathophysiology Division, Lovelace Respiratory Research Institute, Albuquerque, NM 87108, USA
    J Neuroimmunol 83:148-56. 1998
  2. pmc Crucial role of alpha4 and alpha6 nicotinic acetylcholine receptor subunits from ventral tegmental area in systemic nicotine self-administration
    S Pons
    Unité Neurobiologie Intégrative des Systèmes Cholinergiques, Institut Pasteur, 75724 Paris Cedex 15, France
    J Neurosci 28:12318-27. 2008
  3. pmc Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking
    Pia Steensland
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, 5858 Horton Street, Suite 200, Emeryville, CA 94608, USA
    Proc Natl Acad Sci U S A 104:12518-23. 2007
  4. pmc Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysis
    Sonal Singh
    Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, USA
    CMAJ 183:1359-66. 2011
  5. ncbi Nicotinic acetylcholine involvement in cognitive function in animals
    E D Levin
    Department of Psychiatry, Duke University Medical Center, Durham, NC 27710, USA
    Psychopharmacology (Berl) 138:217-30. 1998
  6. ncbi Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations
    Anders A Jensen
    Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK 2100 Copenhagen, Denmark
    J Med Chem 48:4705-45. 2005
  7. ncbi Effects of varenicline on smoking cessation in patients with mild to moderate COPD: a randomized controlled trial
    Donald P Tashkin
    Department of Medicine, David Geffen School of Medicine at University of California, Los Angeles, 10833 Le Conte Ave, Los Angeles, CA 90095 1690, USA
    Chest 139:591-9. 2011
  8. pmc Structural determinants for interaction of partial agonists with acetylcholine binding protein and neuronal alpha7 nicotinic acetylcholine receptor
    Ryan E Hibbs
    Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA, USA
    EMBO J 28:3040-51. 2009
  9. pmc Varenicline reduces alcohol self-administration in heavy-drinking smokers
    Sherry A McKee
    Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut 06519, USA
    Biol Psychiatry 66:185-90. 2009
  10. ncbi Structural and functional diversity of native brain neuronal nicotinic receptors
    Cecilia Gotti
    Department of Medical Pharmacology, CNR, Institute of Neuroscience, Cellular and Molecular Pharmacology, University of Milan, Milan, Italy
    Biochem Pharmacol 78:703-11. 2009

Detail Information

Publications293 found, 100 shown here

  1. ncbi Immunomodulatory effects of cigarette smoke
    M L Sopori
    Pathophysiology Division, Lovelace Respiratory Research Institute, Albuquerque, NM 87108, USA
    J Neuroimmunol 83:148-56. 1998
    ..Nicotine-induced immunosuppression may result from its direct effects on lymphocytes, indirectly through its effects on the neuroendocrine system, or both...
  2. pmc Crucial role of alpha4 and alpha6 nicotinic acetylcholine receptor subunits from ventral tegmental area in systemic nicotine self-administration
    S Pons
    Unité Neurobiologie Intégrative des Systèmes Cholinergiques, Institut Pasteur, 75724 Paris Cedex 15, France
    J Neurosci 28:12318-27. 2008
    ....
  3. pmc Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking
    Pia Steensland
    Ernest Gallo Clinic and Research Center, University of California, San Francisco, 5858 Horton Street, Suite 200, Emeryville, CA 94608, USA
    Proc Natl Acad Sci U S A 104:12518-23. 2007
    ..The selectivity of varenicline in decreasing ethanol consumption combined with its reported safety profile and mild side effects in humans suggest that varenicline may prove to be a treatment for alcohol dependence...
  4. pmc Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysis
    Sonal Singh
    Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD, USA
    CMAJ 183:1359-66. 2011
    ..We conducted a systematic review and meta-analysis of randomized controlled trials to ascertain the serious adverse cardiovascular effects of varenicline compared with placebo among tobacco users...
  5. ncbi Nicotinic acetylcholine involvement in cognitive function in animals
    E D Levin
    Department of Psychiatry, Duke University Medical Center, Durham, NC 27710, USA
    Psychopharmacology (Berl) 138:217-30. 1998
    ..b>Nicotinic agonists have been found in rodent and non-human primate studies to improve performance on a variety of memory tasks...
  6. ncbi Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations
    Anders A Jensen
    Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK 2100 Copenhagen, Denmark
    J Med Chem 48:4705-45. 2005
  7. ncbi Effects of varenicline on smoking cessation in patients with mild to moderate COPD: a randomized controlled trial
    Donald P Tashkin
    Department of Medicine, David Geffen School of Medicine at University of California, Los Angeles, 10833 Le Conte Ave, Los Angeles, CA 90095 1690, USA
    Chest 139:591-9. 2011
    ..To our knowledge, this is the first randomized clinical trial to compare the efficacy and safety of varenicline tartrate vs placebo in smokers with mild to moderate COPD...
  8. pmc Structural determinants for interaction of partial agonists with acetylcholine binding protein and neuronal alpha7 nicotinic acetylcholine receptor
    Ryan E Hibbs
    Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA, USA
    EMBO J 28:3040-51. 2009
    ....
  9. pmc Varenicline reduces alcohol self-administration in heavy-drinking smokers
    Sherry A McKee
    Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut 06519, USA
    Biol Psychiatry 66:185-90. 2009
    ..Varenicline, a partial nicotinic agonist with high affinity for the alpha4beta2 nAChR receptor, reduced ethanol intake in rodents. We aimed to test whether varenicline would reduce alcohol consumption and alcohol craving in humans...
  10. ncbi Structural and functional diversity of native brain neuronal nicotinic receptors
    Cecilia Gotti
    Department of Medical Pharmacology, CNR, Institute of Neuroscience, Cellular and Molecular Pharmacology, University of Milan, Milan, Italy
    Biochem Pharmacol 78:703-11. 2009
    ..We also discuss recent findings concerning the effect of chronic nicotine on the expression of native subtypes...
  11. ncbi In vivo nicotine treatment regulates mesocorticolimbic CREB and ERK signaling in C57Bl/6J mice
    Darlene H Brunzell
    Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut, USA
    J Neurochem 84:1431-41. 2003
    ..Overall, these results support a role for ERK and CREB activity in neural plasticity associated with nicotine dependence...
  12. ncbi Involvement of nicotinic acetylcholine receptors in suppression of antimicrobial activity and cytokine responses of alveolar macrophages to Legionella pneumophila infection by nicotine
    K Matsunaga
    Department of Medical Microbiology and Immunology, University of South Florida College of Medicine, Tampa, FL 33612, USA
    J Immunol 167:6518-24. 2001
    ....
  13. ncbi Pharmacological characterization of recombinant human neuronal nicotinic acetylcholine receptors h alpha 2 beta 2, h alpha 2 beta 4, h alpha 3 beta 2, h alpha 3 beta 4, h alpha 4 beta 2, h alpha 4 beta 4 and h alpha 7 expressed in Xenopus oocytes
    L E Chavez-Noriega
    SIBIA Neurosciences, Inc, La Jolla, California, USA
    J Pharmacol Exp Ther 280:346-56. 1997
    ..h alpha 4 beta 4 and h alpha 7 were expressed in Xenopus oocytes and tested for their sensitivities to the nicotinic agonists acetylcholine (ACh), nicotine, cytisine (CYT) and 1,1-dimethyl-4-phenylpiperazinium (DMPP) and the nAChR...
  14. ncbi Crystal structure of nicotinic acetylcholine receptor homolog AChBP in complex with an alpha-conotoxin PnIA variant
    Patrick H N Celie
    Division of Molecular Carcinogenesis, Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Nat Struct Mol Biol 12:582-8. 2005
    ..Knowledge of these contacts could facilitate the rational design of drug leads using the Ctx framework and may lead to compounds with increased receptor subtype selectivity...
  15. ncbi Varenicline for smoking cessation: a placebo-controlled, randomized study
    Chen Wang
    Department of Epidemiology, Beijing Institute of Respiratory Medicine, WHO Collaborating Center for Tobacco or Health, Beijing Chao Yang Hospital Affiliated, Capital Medical University, Beijing, China
    Respirology 14:384-92. 2009
    ..This study evaluated the efficacy of a standard regimen of varenicline compared with placebo for smoking cessation in 333 subjects in China, Singapore and Thailand...
  16. pmc Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site
    Jaskiran K Gill
    Department of Neuroscience, University College London, London WC1E 6BT, United Kingdom
    Proc Natl Acad Sci U S A 108:5867-72. 2011
    ..Whereas the α7 nAChR antagonist metyllycaconitine acts competitively with conventional nicotinic agonists, metyllycaconitine is a noncompetitive antagonist of 4BP-TQS...
  17. pmc Atomic interactions of neonicotinoid agonists with AChBP: molecular recognition of the distinctive electronegative pharmacophore
    Todd T Talley
    Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California at San Diego, La Jolla, CA 99093 0657, USA
    Proc Natl Acad Sci U S A 105:7606-11. 2008
    ..This template defines the association of interacting amino acids and their energetic contributions to the distinctive interactions of neonicotinoids...
  18. ncbi Smoking behaviour and compensation: a review of the literature
    G Scherer
    ABF Analytisch biologisches Forschungslabor München, Germany
    Psychopharmacology (Berl) 145:1-20. 1999
    ..The issue of compensation is important because it bears on whether switching to "lighter" brands means lower overall smoke intake or not...
  19. ncbi Nicotinic acetylcholine receptors containing alpha 7 subunits on rat cortical neurons do not undergo long-lasting inactivation even when up-regulated by chronic nicotine exposure
    H Kawai
    Neurobiology Section, Division of Biology, University of California, San Diego, La Jolla, California 92093-0357, USA
    J Neurochem 78:1367-78. 2001
    ....
  20. ncbi Regulatory role of the α7nAChR in cancer
    Hildegard M Schuller
    Experimental Oncology Laboratory, Department of Pathobiology, College of Veterinary Medicine, University of Tennessee, 2407 River Drive, Knoxville, TN 37996, USA
    Curr Drug Targets 13:680-7. 2012
    ....
  21. pmc Nicotine induces cell proliferation, invasion and epithelial-mesenchymal transition in a variety of human cancer cell lines
    Piyali Dasgupta
    Drug Discovery Program, H Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA
    Int J Cancer 124:36-45. 2009
    ..Therefore, it is probable that the ability of nicotine to induce invasion and EMT may contribute to the progression of breast and lung cancers...
  22. ncbi Cigarette smoking and diabetes
    Bjorn Eliasson
    Lundberg Laboratory for Diabetes Research, Sahlgrenska University Hospital, Goteborg, Sweden
    Prog Cardiovasc Dis 45:405-13. 2003
    ..In diabetes care, smoking cessation is of utmost importance to facilitate glycemic control and limit the development of diabetic complications...
  23. pmc Identification and characterization of novel nicotinic receptor-associated proteins in Caenorhabditis elegans
    Alexander Gottschalk
    Institute for Biochemistry, Goethe University, Frankfurt, Germany
    EMBO J 24:2566-78. 2005
    ..Thus, tandem affinity purification is a viable approach to identify novel proteins regulating neurotransmitter receptor activity or expression in model systems like C. elegans...
  24. ncbi A review of experimental techniques used for the heterologous expression of nicotinic acetylcholine receptors
    Neil S Millar
    Department of Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, UK
    Biochem Pharmacol 78:766-76. 2009
    ..It will focus, in particular, upon studies of recombinant nAChRs, work that has been conducted by many hundreds of scientists during a period of almost 30 years since the molecular cloning of nAChR subunits in the early 1980s...
  25. pmc Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia
    Carrie K Jones
    Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Neuropsychopharmacology 37:16-42. 2012
    ....
  26. ncbi A double-blind randomized placebo-controlled pilot study of neuropsychiatric adverse events in abstinent smokers treated with varenicline or placebo
    Dahlia Garza
    Pfizer Pharmaceuticals Inc, New York, New York 10017, USA
    Biol Psychiatry 69:1075-82. 2011
    ..There have been spontaneous postmarketing reports of neuropsychiatric adverse events (NPAEs) in smokers without a history of psychiatric illness quitting with varenicline...
  27. pmc Requisite role of the cholinergic alpha7 nicotinic acetylcholine receptor pathway in suppressing Gram-negative sepsis-induced acute lung inflammatory injury
    Xiao Su
    Center for Lung and Vascular Biology and Department of Pharmacology, University of Illinois at Chicago, Chicago, IL 60612, USA
    J Immunol 184:401-10. 2010
    ..coli-induced ALI by reducing chemokine production and transalveolar neutrophil migration, suggesting that activation of alpha7 nAChR may be a promising strategy for treatment of sepsis-induced ALI...
  28. pmc Activation of alpha4* nAChRs is necessary and sufficient for varenicline-induced reduction of alcohol consumption
    Linzy M Hendrickson
    Brudnick Neuropsychiatric Research Institute, and Program in Neuroscience, University of Massachusetts Medical School, 303 Belmont Street, Worcester, MA 01604, USA
    J Neurosci 30:10169-76. 2010
    ..Together, our data indicate that activation of alpha4* nAChRs is necessary and sufficient for varenicline reduction of alcohol consumption...
  29. pmc Effects of an alpha 7-nicotinic agonist on default network activity in schizophrenia
    Jason R Tregellas
    Department of Psychiatry, Denver VA Medical Center, VISN19 MIRECC, Colorado, USA
    Biol Psychiatry 69:7-11. 2011
    ..This study examined the effects of DMXB-A on default network activity as a biomarker for drug effects on pathologic brain function associated with schizophrenia...
  30. ncbi Efficacy and safety of nicotine replacement therapy for smoking cessation in pregnancy: systematic review and meta-analysis
    Tim Coleman
    UK Centre for Tobacco Control Studies, University of Nottingham, Medical School, Nottingham, UK
    Addiction 106:52-61. 2011
    ..To determine the efficacy and safety of nicotine replacement therapy (NRT) with or without behavioural support when used to support smoking cessation in pregnancy...
  31. ncbi Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures
    Patrick H N Celie
    Division of Molecular Carcinogenesis, Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Neuron 41:907-14. 2004
    ..These structures will be useful tools for the development of new drugs involving nicotinic acetylcholine receptor-associated diseases...
  32. ncbi Nicotine gates long-term potentiation in the hippocampal CA1 region via the activation of alpha2* nicotinic ACh receptors
    Sakura Nakauchi
    Department of Neurobiology and Behaviour, University of California, Irvine, CA 92697 4550, USA
    Eur J Neurosci 25:2666-81. 2007
    ..These effects of nicotine may represent the cellular basis of nicotine-mediated cognitive enhancement...
  33. ncbi Nicotine modulates reorienting of visuospatial attention and neural activity in human parietal cortex
    Christiane M Thiel
    Institute of Medicine, Research Centre Julich, Julich, Germany
    Neuropsychopharmacology 30:810-20. 2005
    ..We conclude that nicotine enhances reorienting of attention in visuospatial tasks and that one behavioral correlate of speeded RTs is reduced parietal activity...
  34. ncbi Cue dependency of nicotine self-administration and smoking
    A R Caggiula
    Department of Psychology, 455 Langley Hall, University of Pittsburgh, Pittsburgh, PA 15260, USA
    Pharmacol Biochem Behav 70:515-30. 2001
    ....
  35. ncbi Time-dependent changes in transcriptional profiles within five rat brain regions in response to nicotine treatment
    Ming D Li
    Program in Genomics and Bioinformatics on Drug Abuse, Department of Psychiatry, The University of Texas Health Science Center, MSC 7792, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States
    Brain Res Mol Brain Res 132:168-80. 2004
    ..Using a systematic approach to compare the different regional responses to nicotine administration will eventually provide a better understanding of how the different brain regions responding to this drug...
  36. ncbi Long-lasting cognitive improvement with nicotinic receptor agonists: mechanisms of pharmacokinetic-pharmacodynamic discordance
    Jerry J Buccafusco
    Department of Pharmacology and Toxicology, Alzheimer s Research Center, Medical College of Georgia, Augusta, GA 30912, USA
    Trends Pharmacol Sci 26:352-60. 2005
    ..A better understanding of this phenomenon might shed new light on the role of nAChR systems in memory formation and retrieval...
  37. ncbi Adherence to nicotine replacement therapy versus quitting smoking among Chinese smokers: a preliminary investigation
    Tai Hing Lam
    Department of Community Medicine, The University of Hong Kong, Hong Kong, China
    Psychopharmacology (Berl) 177:400-8. 2005
    ..There are over 300 million Chinese smokers, but use of nicotine replacement therapy (NRT) is rare. On the other hand, data on the factors associated with quitting and adherence to NRT use are scarce in the East...
  38. ncbi Cognitive improvement by activation of alpha7 nicotinic acetylcholine receptors: from animal models to human pathophysiology
    Morten S Thomsen
    Neurobiology Research Unit, Copenhagen University Hospital, Copenhagen, Denmark
    Curr Pharm Des 16:323-43. 2010
    ..It is therefore important to consider the translational power of the animal models used before entering into a clinical evaluation of the pro-cognitive effects of alpha(7) nAChR activation...
  39. ncbi Recent advances in Cys-loop receptor structure and function
    Steven M Sine
    Department of Physiology, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA
    Nature 440:448-55. 2006
    ..Namely, analyses of disease-causing mutations have clarified receptor structure-function relationships as well as mechanisms governing the postsynaptic response...
  40. ncbi Nicotine patch therapy prior to quitting smoking: a meta-analysis
    Saul Shiffman
    Pinney Associates, Pittsburgh, PA 15213, USA
    Addiction 103:557-63. 2008
    ..To evaluate the incremental efficacy of starting nicotine patch treatment prior to quitting compared to the current regimen of starting patch treatment on the target quit day...
  41. ncbi Neurochemical and behavioral studies on ethanol and nicotine interactions
    Anna Larsson
    Department of Pharmacology, Goteborg University, Box 431, Göteborg SE 405 30, Sweden
    Neurosci Biobehav Rev 27:713-20. 2004
    ....
  42. ncbi Nicotine potentiation of brain stimulation reward reversed by DH beta E and SCH 23390, but not by eticlopride, LY 314582 or MPEP in rats
    Amanda A Harrison
    Department of Neuropharmacology, The Scripps Research Institute, La Jolla, CA 92037, USA
    Psychopharmacology (Berl) 160:56-66. 2002
    ..Nicotine-induced increases of dopamine in the nucleus accumbens are in part mediated by glutamatergic projections to the ventral tegmental area dopamine neurons...
  43. ncbi Binding and functional activity of nicotinic cholinergic receptors in selected rat brain regions are increased following long-term but not short-term nicotine treatment
    Henry N Nguyen
    Department of Pharmacology and Physiology, and Institute for Biomedical Sciences, George Washington University, Washington, DC, USA
    J Neurochem 90:40-9. 2004
    ..91), suggesting that rat brain receptors up-regulated by chronic nicotine are active. These results have important consequences for understanding nicotinic receptor neurobiology in smokers and users of nicotine replacement therapy...
  44. ncbi Temporal change in human nicotinic acetylcholine receptor after smoking cessation: 5IA SPECT study
    Marcelo Mamede
    Department of Diagnostic Imaging and Nuclear Medicine, Graduate School of Medicine, Kyoto University, Kyoto, Japan
    J Nucl Med 48:1829-35. 2007
    ..However, changes in nAChRs after cigarette smoking cessation in humans are poorly understood. The aim of this study was to detect the dynamic changes of nAChRs after smoking and smoking cessation in the brains of living subjects...
  45. ncbi Nicotinic receptor subtypes and cognitive function
    Edward D Levin
    Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Neurobehavioral Research Laboratory, Box 3412, Durham, North Carolina 27710, USA
    J Neurobiol 53:633-40. 2002
    ..These studies of the neural nicotinic mechanisms underlying cognitive function are key for opening avenues for development of safe and effective nicotinic treatments for cognitive dysfunction...
  46. ncbi Post-training intrahippocampal infusion of nicotine prevents spatial memory retention deficits induced by the cyclo-oxygenase-2-specific inhibitor celecoxib in rats
    Mohammad Sharifzadeh
    Department of Toxicology and Pharmacology, School of Pharmacy, Pharmaceutical Sciences and Medicinal Plant Research Centers, University of Medical Sciences, Tehran, Iran
    J Neurochem 95:1078-90. 2005
    ..These results suggest that nicotine prevented or reversed the adverse effects of celecoxib on spatial memory retention and protected or restored the immunostaining pattern of COX-2 neurons in the rat dorsal hippocampus...
  47. ncbi Desensitized nicotinic receptors in brain
    Hai Wang
    Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P R China
    Brain Res Brain Res Rev 48:420-37. 2005
    ..These studies provide the critical information for understanding the importance of nicotinic receptors desensitization in both normal physiological processing and in various disease states...
  48. ncbi Transdermal nicotine attenuates depression symptoms in nonsmokers: a double-blind, placebo-controlled trial
    F Joseph McClernon
    Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC, USA
    Psychopharmacology (Berl) 189:125-33. 2006
    ..Despite established links between nicotine dependence and depression, little research has examined the effects of nicotine on depression symptoms...
  49. pmc Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations
    Scott B Hansen
    Department of Pharmacology, University of California at San Diego, La Jolla, CA 92093 0636, USA
    EMBO J 24:3635-46. 2005
    ..This comprehensive set of structures reflects a dynamic template for delineating further conformational changes of the LBD of the nicotinic receptor...
  50. ncbi α7 nicotinic acetylcholine receptor subunit in angiogenesis and epithelial to mesenchymal transition
    Smitha Pillai
    Department of Tumor Biology, H Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Mail Code SRB3, Tampa, FL 33647, USA
    Curr Drug Targets 13:671-9. 2012
    ..These observations on nicotine function highlight the therapeutic potential of α7nAChR agonists and antagonists for combating angiogenesis related diseases...
  51. pmc A series of α7 nicotinic acetylcholine receptor allosteric modulators with close chemical similarity but diverse pharmacological properties
    Jaskiran K Gill
    Department of Neuroscience, Physiology and Pharmacology, University College London, London, UK
    Mol Pharmacol 81:710-8. 2012
    ..These findings provide evidence of the pharmacological diversity of compounds interacting with the allosteric transmembrane site on α7 nAChRs...
  52. ncbi Nicotine-induced upregulation of human neuronal nicotinic alpha7-receptors is potentiated by modulation of cAMP and PKC in SH-EP1-halpha7 cells
    Saara Nuutinen
    Division of Pharmacology and Toxicology, Faculty of Pharmacy, P O Box 56 Viikinkaari 5 E, University of Helsinki, FIN 00014, Finland
    Eur J Pharmacol 544:21-30. 2006
    ....
  53. pmc Attenuation of CNS inflammatory responses by nicotine involves α7 and non-α7 nicotinic receptors
    Junwei Hao
    Division of Neurology, St Joseph s Hospital and Medical Center, Phoenix, AZ 85013, USA
    Exp Neurol 227:110-9. 2011
    ....
  54. ncbi Schizophrenia and the alpha7 nicotinic acetylcholine receptor
    Laura F Martin
    Research Service, VA Eastern Colorado Health Care System, Denver, Colorado 80220, USA
    Int Rev Neurobiol 78:225-46. 2007
    ..alpha7 Nicotinic acetylcholine receptor agonists appear to be viable candidates for the treatment of cognitive disturbances in schizophrenia...
  55. ncbi Nicotinic acetylcholine receptors in the mesolimbic pathway: primary role of ventral tegmental area alpha6beta2* receptors in mediating systemic nicotine effects on dopamine release, locomotion, and reinforcement
    Cecilia Gotti
    Department of Medical Pharmacology, Consiglio Nazionale delle Ricerche, Institute of Neuroscience, Cellular and Molecular Pharmacology Center, University of Milan, 20129 Milan, Italy
    J Neurosci 30:5311-25. 2010
    ....
  56. pmc Intrathecal injection of an alpha seven nicotinic acetylcholine receptor agonist attenuates gp120-induced mechanical allodynia and spinal pro-inflammatory cytokine profiles in rats
    Lisa C Loram
    Department of Psychology and Neuroscience, University of Colorado, Boulder, CO 80309, USA
    Brain Behav Immun 24:959-67. 2010
    ..Taken together, the data support that alpha7nAchR may be a novel target for treating pain where microglia maintain the pro-inflammatory state within the spinal cord...
  57. ncbi Effect of varenicline and bupropion SR on craving, nicotine withdrawal symptoms, and rewarding effects of smoking during a quit attempt
    Robert West
    Cancer Research UK Health Behaviour Unit, Department of Epidemiology and Public Health, University College London, Brook House, London, UK
    Psychopharmacology (Berl) 197:371-7. 2008
    ....
  58. ncbi Localization of agonist and competitive antagonist binding sites on nicotinic acetylcholine receptors
    H R Arias
    Instituto de Matemática de Bahía Blanca, Consejo Nacional de Investigaciones Científicas y Técnicas CONICET and Universidad Nacional del Sur, Av Alem 1253, 8000 Bahia Blanca, Argentina
    Neurochem Int 36:595-645. 2000
    ..which includes loop E), and residues gammaL(119) (close to loop F) and gammaE(176) (close to loop G) at the low-affinity binding site, or deltaL(121) (close to the homologous region of loop G) at the high-affinity binding site, are i..
  59. pmc It is not "either/or": activation and desensitization of nicotinic acetylcholine receptors both contribute to behaviors related to nicotine addiction and mood
    Marina R Picciotto
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06508, USA
    Prog Neurobiol 84:329-42. 2008
    ..We conclude that there are effects of nAChR activation and desensitization on drug reinforcement and affective behavior, and that both processes are important in the behavioral consequences of nicotine in tobacco smoking...
  60. ncbi Mechanisms of nicotine actions on dorsal raphe serotoninergic neurons
    Stefan Mihailescu
    Facultad de Medicina, Departamento de Fisiologia, Instituto de Fisiologia Celular, UNAM, Mexico City, Mexico DF, Mexico
    Eur J Pharmacol 452:77-82. 2002
    ....
  61. pmc An integrated catch-and-hold mechanism activates nicotinic acetylcholine receptors
    Snehal Jadey
    Department of Physiology and Biophysics, State University of New York, Buffalo, NY 14214, USA
    J Gen Physiol 140:17-28. 2012
    ..The catch-and-hold reaction coordinate is discussed in terms of preopening states and thermodynamic cycles of activation...
  62. pmc Population pharmacokinetic analysis of varenicline in adult smokers
    Patanjali Ravva
    Global Pharmacometrics, Primary Care Business Unit, Worldwide Pharmaceutical Operations, Pfizer Inc, New London, Connecticut 06320, USA
    Br J Clin Pharmacol 68:669-81. 2009
    ..To characterize the population pharmacokinetics of varenicline and identify factors leading to its exposure variability in adult smokers...
  63. ncbi Nicotine enhances sustained attention in the rat under specific task conditions
    N R Mirza
    Section of Behavioural Pharmacology, Institute of Psychiatry, London, UK
    Psychopharmacology (Berl) 138:266-74. 1998
    ..attention may reflect self-reports by smokers that nicotine aids concentration, particularly in stressful situations, and (iii) nicotinic agonists may have therapeutic benefits in patient populations suffering from attentional deficits.
  64. ncbi Use of varenicline for 4 weeks before quitting smoking: decrease in ad lib smoking and increase in smoking cessation rates
    Peter Hajek
    United Kingdom Centre for Tobacco Control Studies, Wolfson Institute of Preventive Medicine, Barts and the London School of Medicine and Dentistry, Queen Mary, University of London, London, England
    Arch Intern Med 171:770-7. 2011
    ..We set out to determine whether increasing the prequit medication period renders cigarettes less satisfying and facilitates quitting...
  65. pmc A randomized placebo-controlled trial of varenicline for smoking cessation allowing flexible quit dates
    Stephen Rennard
    Division of Pulmonary, Critical Care, Sleep and Allergy, University of Nebraska Medical Center, Omaha, NE 68198 5910, USA
    Nicotine Tob Res 14:343-50. 2012
    ..The objective of this study was to compare varenicline 1 mg twice daily (b.i.d.) with placebo in subjects using a flexible quit date paradigm after starting medication...
  66. ncbi Antidepressant effect of ingested nicotine in female rats of Flinders resistant and sensitive lines
    V J Djurić
    Father Sean O Sullivan Research Centre, St Joseph s Hospital, Department of Psychiatry and Behavioral Neurosciences, McMaster University, Hamilton, Ontario, Canada
    Physiol Behav 67:533-7. 1999
    ..Animal studies on nicotine ingestion and withdrawal may become an important source of insights into the comorbidity of depression and nicotine self-administration...
  67. ncbi Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them
    Yingxian Xiao
    Department of Pharmacology, Georgetown University School of Medicine, Washington, DC 20057, USA
    Mol Pharmacol 70:1454-60. 2006
    ..effects of sazetidine-A and nicotine at alpha4beta2 nAChRs suggests that the predominant effects of nicotine and other nicotinic agonists are related to desensitization of the receptors and that sazetidine-A potently mimics these effects.
  68. ncbi Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applications
    M Novella Romanelli
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Gino Capponi 9, 50121 Firenze, Italy
    Med Res Rev 23:393-426. 2003
    ..This review focuses on the structure of new ligands for nAChRs, agonists, antagonists and allosteric modulators, and on their possible applications...
  69. ncbi Methyllycaconitine is a potent antagonist of alpha-conotoxin-MII-sensitive presynaptic nicotinic acetylcholine receptors in rat striatum
    Adrian J Mogg
    Department of Biology and Biochemistry, University of Bath, Bath BA2 7AY, United Kingdom
    J Pharmacol Exp Ther 302:197-204. 2002
    ..The use of MLA as an alpha7-selective antagonist should be exercised with caution, especially in studies of nAChR in basal ganglia...
  70. pmc Varenicline is a potent agonist of the human 5-hydroxytryptamine3 receptor
    S C R Lummis
    Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1QW, United Kingdom
    J Pharmacol Exp Ther 339:125-31. 2011
    ..Therefore, activation of human 5-HT(3) receptors may be responsible for some of the side effects that preclude use of higher doses during varenicline treatment...
  71. pmc Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect
    Hans Rollema
    Department Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
    Eur J Pharmacol 605:114-6. 2009
    ..These data suggest that varenicline may have antidepressant potential and can, when combined, augment antidepressant responses of selective serotonin reuptake inhibitors...
  72. pmc Pre-synaptic nicotinic receptors evoke endogenous glutamate and aspartate release from hippocampal synaptosomes by way of distinct coupling mechanisms
    S Zappettini
    Department of Experimental Medicine, Section of Pharmacology and Toxicology Center of Excellence for Biomedical Research National Institute of Neuroscience, University of Genoa, Viale Cembrano 4, Genoa, Italy
    Br J Pharmacol 161:1161-71. 2010
    ..The present work aimed to investigate whether and through which mechanisms selective α7 and α4β2 nicotinic receptor (nAChR) agonists stimulate endogenous glutamate (GLU) and aspartate (ASP) release in rat hippocampus...
  73. ncbi Transgenic mice over-expressing human beta-amyloid have functional nicotinic alpha 7 receptors
    J P Spencer
    Neurology and GI CEDD, GlaxoSmithKline, Harlow, Essex CM19 5AW, UK
    Neuroscience 137:795-805. 2006
    ..Despite this clear inhibition of recombinant receptors, hippocampal GABAergic interneurones in slices from beta-amyloid over-expressing mice still possess alpha 7 receptor-mediated currents...
  74. ncbi What makes for an effective stop-smoking service?
    Leonie S Brose
    NHS Centre for Smoking Cessation and Training NCSCT, University College London, 1 19 Torrington Place, London WC1E 7HB, UK
    Thorax 66:924-6. 2011
    ..However, success varies considerably across services, making it important to examine the factors that influence their effectiveness...
  75. pmc Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380
    Barbara J Caldarone
    PsychoGenics, Inc, 765 Old Saw Mill River Road, Tarrytown, NY 10591, USA
    Psychopharmacology (Berl) 217:199-210. 2011
    ..Nicotinic acetylcholine receptor (nAChR) agonists, partial agonists, and antagonists have antidepressant-like effects in rodents and reduce symptoms of depression in humans...
  76. pmc Cytisine, a partial agonist of high-affinity nicotinic acetylcholine receptors, has antidepressant-like properties in male C57BL/6J mice
    Yann S Mineur
    Department of Psychiatry, Yale University School of Medicine, 34 Park Street, 3rd Floor Research, New Haven, CT 06508, USA
    Neuropharmacology 52:1256-62. 2007
    ..These studies also suggest that both antagonists and partial agonists of alpha4/beta2*nAChRs would be interesting targets for the development of novel antidepressant drugs...
  77. ncbi Tobacco dependence treatment for hospitalized smokers: a randomized, controlled, pilot trial using varenicline
    Michael B Steinberg
    Division of General Internal Medicine, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School, 125 Paterson Street, Suite 2304, New Brunswick, NJ 08903, USA
    Addict Behav 36:1127-32. 2011
    ..This is the first randomized, double-blinded, placebo-controlled pilot trial utilizing varenicline and post-discharge, in-person behavioral treatment for hospitalized smokers...
  78. ncbi Nicotinic receptor-mediated enhancement of long-term potentiation involves activation of metabotropic glutamate receptors and ryanodine-sensitive calcium stores in the dentate gyrus
    Philip Welsby
    Department of Physiology, Trinity College, Dublin 2, Ireland
    Eur J Neurosci 24:3109-18. 2006
    ....
  79. ncbi Characterization of 2-[[4-fluoro-3-(trifluoromethyl)phenyl]amino]-4-(4-pyridinyl)-5-thiazolemethanol (JNJ-1930942), a novel positive allosteric modulator of the {alpha}7 nicotinic acetylcholine receptor
    Theo Dinklo
    Johnson and Johnson Pharmaceutical Research and Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340 Beerse, Belgium
    J Pharmacol Exp Ther 336:560-74. 2011
    ..JNJ-1930942 will be a useful tool to study the therapeutic potential of α(7) nAChR potentiation in central nervous system disorders in which a deficit in α(7) nAChR neurotransmission is hypothesized to be involved...
  80. pmc The safety and efficacy of varenicline in cocaine using smokers maintained on methadone: a pilot study
    James Poling
    Yale University School of Medicine, VA Connecticut Healthcare System, West Haven, Connecticut 06516, USA
    Am J Addict 19:401-8. 2010
    ..These preliminary findings may point to potential therapeutic value of varenicline for smoking cessation in cocaine users maintained on methadone...
  81. ncbi An update on therapeutics for tobacco dependence
    Tim Lancaster
    University of Oxford, Cochrane Tobacco Addiction Review Group, Department of Primary Healthcare, Old Road, Headington, Oxford, OX3 7LF, UK
    Expert Opin Pharmacother 9:15-22. 2008
    ..Recent evidence suggests that the nicotine-receptor partial agonist varenicline is at least as effective as nicotine replacement therapy and antidepressants...
  82. pmc A randomized, controlled trial of NRT-aided gradual vs. abrupt cessation in smokers actively trying to quit
    John R Hughes
    University of Vermont, Burlington, VT, USA
    Drug Alcohol Depend 111:105-13. 2010
    ..One liability of gradual reduction may be that it allows smokers to delay their quit date...
  83. pmc Nicotinic alpha7- or beta2-containing receptor knockout: effects on radial-arm maze learning and long-term nicotine consumption in mice
    Edward D Levin
    Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC 27710, USA
    Behav Brain Res 196:207-13. 2009
    ....
  84. pmc Nicotinic partial agonists varenicline and sazetidine-A have differential effects on affective behavior
    Jill R Turner
    Department of Pharmacology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Pharmacol Exp Ther 334:665-72. 2010
    ..These results suggest that the partial agonists varenicline and sazetidine-A may have diverse therapeutic benefits in affective disorders...
  85. pmc The Drosophila nicotinic acetylcholine receptor subunits Dα5 and Dα7 form functional homomeric and heteromeric ion channels
    Stuart J Lansdell
    Department of Neuroscience, Physiology and Pharmacology, University College London, London, UK
    BMC Neurosci 13:73. 2012
    ..The focus of the present study is the Dα5, Dα6 and Dα7 subunits, which are distinguished by their sequence similarity to one another and also by their close similarity to the vertebrate α7 nAChR subunit...
  86. ncbi Metabotropic glutamate 5 receptor antagonist MPEP decreased nicotine and cocaine self-administration but not nicotine and cocaine-induced facilitation of brain reward function in rats
    P J Kenny
    The Scripps Research Institute, Department of Neuropharmacology, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Ann N Y Acad Sci 1003:415-8. 2003
  87. ncbi Acute beta-amyloid administration disrupts the cholinergic control of dopamine release in the nucleus accumbens
    Stefania Preda
    Department of Experimental and Applied Pharmacology, Centre of Excellence in Applied Biology, University of Pavia, Pavia, Italy
    Neuropsychopharmacology 33:1062-70. 2008
    ..Also the nicotinic agonists epibatidine and nicotine evoked a dopaminergic outflow in nucleus accumbens, which, however, was lower...
  88. pmc A preliminary investigation of varenicline for heavy drinking smokers
    Lisa M Fucito
    Department of Psychiatry, CMHC S200, Yale University School of Medicine, 34 Park Street, New Haven, CT 06519, USA
    Psychopharmacology (Berl) 215:655-63. 2011
    ..However, varenicline has not been tested in heavy drinkers, and it remains to be determined whether varenicline could reduce alcohol craving and consumption in smokers who are trying to quit smoking...
  89. pmc Behavioral counseling and varenicline treatment for smoking cessation
    Gary E Swan
    SRI International, Menlo Park, California 94025, USA
    Am J Prev Med 38:482-90. 2010
    ..Smoking remains the primary preventable cause of death and illness in the U.S. Effective, convenient treatment programs are needed to reduce smoking prevalence...
  90. ncbi Nicotine effects on brain function and functional connectivity in schizophrenia
    Leslie K Jacobsen
    Department of Psychiatry, Yale University School of Medicine, 100 York Street 28, West Haven, CT 06511, USA
    Biol Psychiatry 55:850-8. 2004
    ..Our primary aim was to determine whether nicotine improves cognitive function by facilitating activation of brain regions mediating task performance or by facilitating functional connectivity...
  91. pmc Nicotine accelerates angiogenesis and wound healing in genetically diabetic mice
    Johannes Jacobi
    Division of Cardiovascular Medicine, Stanford University School of Medicine, Stanford, CA 94305, USA
    Am J Pathol 161:97-104. 2002
    ..We have discovered a cholinergic pathway for angiogenesis that is involved in wound healing, and which is a potential target for therapeutic angiogenesis...
  92. ncbi Nicotine withdrawal induces subsensitivity of hypothalamic-pituitary-adrenal axis to stress in rats: implications for precipitation of depression during smoking cessation
    J Semba
    Division of Health Sciences, University of the Air, 2 11 Wakaba, Mihama ku, Chiba 261 8586, Japan
    Psychoneuroendocrinology 29:215-26. 2004
    ....
  93. ncbi fMRI data predict individual differences of behavioral effects of nicotine: a partial least square analysis
    C Giessing
    Institute of Neuroscience and Biophysics, Research Centre Julich, Julich, Germany
    J Cogn Neurosci 19:658-70. 2007
    ....
  94. ncbi Ethnic differences in N-glucuronidation of nicotine and cotinine
    N L Benowitz
    Division of Clinical Pharmacology and Experimental Therapeutics, Medical Service, San Francisco General Hospital Medical Center, University of California, San Francisco, 94143 1220, USA
    J Pharmacol Exp Ther 291:1196-203. 1999
    ..Ethnic differences in the metabolism of other drugs undergoing N-glucuronidation should be studied...
  95. ncbi Effects of the cholinergic agonist nicotine on reorienting of visual spatial attention and top-down attentional control
    C M Thiel
    Department of Medicine, Institute of Neuroscience and Biophysics, Research Centre Juelich, 52425 Juelich, Germany
    Neuroscience 152:381-90. 2008
    ..In contrast, the findings in the occipital cortex do not support the hypothesis that the effects of nicotine on attentional reorienting are due to reduced reliance on top-down information derived from prior cues...
  96. ncbi C957T polymorphism of the dopamine D2 receptor gene modulates the effect of nicotine on working memory performance and cortical processing efficiency
    Leslie K Jacobsen
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06519, USA
    Psychopharmacology (Berl) 188:530-40. 2006
    ....
  97. ncbi Nicotinic involvement in memory function in zebrafish
    Edward D Levin
    Neurobehavioral Research Laboratory, Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC, USA
    Neurotoxicol Teratol 26:731-5. 2004
    ..This study shows that nicotine affects memory function in zebrafish much like in rats, mice, monkeys and humans. Now, zebrafish can be used to help understand the molecular mechanisms crucial to nicotine effects on memory...
  98. pmc Partial agonists of the α3β4* neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in rats
    Susmita Chatterjee
    Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA 94608, USA
    Neuropsychopharmacology 36:603-15. 2011
    ..CP-601932 has been shown to be safe in humans and may represent a potential novel treatment for AUDs...
  99. ncbi Combination treatment with varenicline and nicotine replacement therapy
    Jon O Ebbert
    Mayo Clinic College of Medicine, 200 1st Street Southwest, Rochester, MN 55905, USA
    Nicotine Tob Res 11:572-6. 2009
    ..A paucity of data exists regarding the safety and effectiveness of combination treatment with varenicline and nicotine replacement therapy (NRT)...
  100. ncbi Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis
    Chris Ulens
    Division of Molecular Carcinogenesis, Netherlands Cancer Institute, Amsterdam, The Netherlands
    J Med Chem 52:2372-83. 2009
    ..The analysis of the dual binding mode of these dibenzosuberyl-containing compounds can lead to better understanding of the complex mode of action of similar tricyclic ligands on Cys-loop receptors...
  101. ncbi Intracellular Ca2+ signals evoked by stimulation of nicotinic acetylcholine receptors in SH-SY5Y cells: contribution of voltage-operated Ca2+ channels and Ca2+ stores
    Federico A Dajas-Bailador
    Department of Biology and Biochemistry, University of Bath, Bath, UK
    J Neurochem 81:606-14. 2002
    ..Moreover, the alpha7, but not alpha3beta2* nAChR, are responsible for a fraction of the VOCC-independent nicotine-evoked Ca2+ increase that appears to be functionally coupled to ryanodine sensitive Ca2+ stores...

Research Grants65

  1. Nicotine, nicotinic receptors and lung cancer
    Eliot R Spindel; Fiscal Year: 2013
    ....
  2. Interventions to Test the alpha 7 Nicotinic Receptor Model in Schizophrenia
    Stephen Deutsch; Fiscal Year: 2009
    ..This hypothesis has stimulated both preclinical and clinical exploration of nicotinic agonists to enhance functioning of the receptor...
  3. fMRI of Cholinergic Mechanisms in Schizophrenia
    Jason R Tregellas; Fiscal Year: 2013
    ....
  4. Studies with Nicotinic Null Mutant Mice
    Michael J Marks; Fiscal Year: 2013
    ..a10 and, with the exception of a5, provide the binding site for nicotine and other nicotinic agonists. The three remaining subunits, [unreadable]2-[unreadable]4, are referred to as structural subunits...
  5. Basic to Clinical Molecular Neurobiology of Nicotinic Receptors in Schizophrenia
    Robert Freedman; Fiscal Year: 2013
    ..The Center investigates the potential therapeutic effects of selective alpha 7 nicotinic agonists in animal models of neuronal dysfunction in schizophrenia and then in early human clinical trials in ..
  6. Human Trial of Allosteric Modulator Alpha7 Nicotinic Receptors in Schizophrenia
    Robert Freedman; Fiscal Year: 2013
    ..3) pharmacological evidence for possible therapeutic effects of nicotine as well as more specific alpha7-nicotinic agonists. The hypothesis that emerges is that persons with schizophrenia have diminished expression of the alpha7-..
  7. Proof-of-Concept Trial of an Alpha-7 Nicotinic Agonist for Nicotine Dependence
    Maurizio Fava; Fiscal Year: 2013
    ..In this study, we aim to discover whether a novel treatment will work alone or in combination with nicotine replacement to aid cessation and reduce relapse by minimizing nicotine withdrawal- induced cognitive impairment ..
  8. Nicotinic Agonist in Shizophrenia
    Robert Freedman; Fiscal Year: 2010
    ..We are studying a new, nicotine-like drug, that does not have the harmful effects of tobacco, but may help persons with schizophrenia to think better. ..
  9. Neuronal nicotinic receptor modulation and cerebellar ataxias
    Lynn Wecker; Fiscal Year: 2013
    ..of distinct pathogenic etiology, and preclinical studies have provided proof-of-principle for the use of nicotinic agonists in ataxia, but the mechanism(s) involved have not been elucidated...
  10. Nicotinic Modulation of Methamphetamine's Behavioral and Neurochemical Effects
    RAJEEV INDRAJIT DESAI; Fiscal Year: 2010
    ..Based on reports in the scientific literature and our own preliminary results, nicotinic agonists can interfere with the expression of behavioral and neurochemical effects of MA, and therefore, may be ..
  11. Mechanisms of nicotine-mediated decrease in L-dopa induced-dyskinesias
    Maryka Quik; Fiscal Year: 2013
    ..Treatment with nicotine, or select nicotinic agonists, represents a novel approach to reduce dyskinesias and could lead to the development of new strategies to ..
  12. Nicotinic Receptor Effects on Neurophysiology of Dorsolateral Prefrontal Cortex
    Min Wang; Fiscal Year: 2013
    ..b>Nicotinic agonists have great potential as cognitive enhancers if agents can be found that strengthen PFC without engaging ..
  13. Nicotinic Receptors and Schizophrenia
    Robert Freedman; Fiscal Year: 2013
    ..The hypothesis to be tested in the proposed renewal is that DMXB-A will produce significant neurocognitive improvement in Veterans with schizophrenia. ..
  14. Sensitivity to intravenous nicotine: genetic moderators
    MEHMET contact SOFUOGLU; Fiscal Year: 2010
    ..By providing a better understanding of biological mechanisms of nicotine reward, this study may contribute to development of more effective treatments for smoking cessation. ..
  15. Drug Abuse Methodology: Training and Interdisciplinary Application
    RAJEEV INDRAJIT DESAI; Fiscal Year: 2013
    ..In addition, the planned studies may lead to the further development of promising novel nicotinic-based pharmacotherapy to help combat the scourge of stimulant addiction that plagues our public health. ..
  16. Dose ranging study of varenicline on human alcohol self-administration behavior
    SHERRY ANN MCKEE; Fiscal Year: 2011
    ....
  17. NEUROPEPTIDE Y MODULATION OF ADRENOMEDULLARY SECRETION
    TERRY HEXUM; Fiscal Year: 1993
    ..NPY influence on secretion will be determined by studying it's action in the presence of various nicotinic agonists, it's action on agents stimulating secretion through other than nicotinic receptors and the effect of ..
  18. Cellular Electrophysiology of Nicotine Addiction Clinical Phenotypes
    PATRICIO O'DONNELL; Fiscal Year: 2013
    ..Our goal is to test that neuronal electrophysiological response to nicotinic agonists will be associated with the strength of the clinical imaging based circuit phenotype in patients with severe ..
  19. CHOLINERGIC MECHANISMS OF REM SLEEP GENERATION
    HELEN BAGHDOYAN; Fiscal Year: 1993
    ..nicotinic cholinergic receptors are also involved in REM sleep generation will be tested by administering nicotinic agonists and antagonists and quantifying the effects on REM sleep...
  20. Smoking Cessation and Smoking Relapse Prevention in Patients with Schizophrenia
    A Eden Evins; Fiscal Year: 2010
    ..Participants will then discontinue study medications and enter a 3-month follow up. The primary outcome measure will be 7-day point prevalence abstinence rate at 12 months in the intervention vs. placebo groups. ..
  21. Transdermal Nicotine Treatment of MCI
    Paul Newhouse; Fiscal Year: 2007
    ..Stimulation of nicotinic receptors with nicotine or and/or novel nicotinic agonists reliably improves certain aspects of attentional and memory functioning in both normal individuals, patients ..
  22. Rescue of Chga knockout phenotype by CHGA-BAC transgene
    Sucheta Vaingankar; Fiscal Year: 2009
    ..3. Finally, the CGA variants will be assessed for processing by proteases in vitro and in vivo. ..
  23. NEUROCHEMICAL MECHANISMS OF NICOTINE ACTION
    Cecilia Hillard; Fiscal Year: 1992
    ..3) Monoamines are known to be released by nicotinic agonists. The mechanism of this release will be studied, with particular attention to the involvement of sodium and ..
  24. Nicotinic Receptors in Septally Innervated Hippocampus
    EDSON ALBUQUERQUE; Fiscal Year: 2004
    ..Recently, clinical trials have shown that nicotinic agonists (including nicotine) and drugs that allosterically potentiate the activity of nAChRs are more effective for ..
  25. STIMULUS/TRANSCRIPTION COUPLING IN SYMPATHOADRENAL CELLS
    DANIEL O CONNOR; Fiscal Year: 1999
    ....
  26. Behavioral Genetics and Toxic Response
    Edward Levin; Fiscal Year: 2002
    ....
  27. Adolescence: A Sensitive Period for Nicotine Addiction
    Edward Levin; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  28. Marine Toxin Impacts on Neurobehavioral Function
    Edward Levin; Fiscal Year: 2003
    ..The forum will provide an opportunity for methodological and theoretical issues to be integrated in the context of each talk as well as in a discussion session at the end of the symposium. ..
  29. Nicotinic-Antipsychotic Drug Interactions and Cognition
    Edward Levin; Fiscal Year: 2006
    ..abstract_text> ..
  30. NICOTINIC RECEPTORS IN CEREBRAL CORTICAL DEVELOPMENT
    ALLAN SCHNEIDER; Fiscal Year: 2002
    ..The results of this project will lay the groundwork for further exploration of the role of nicotinic receptors in normal development and that of nicotine as a neuroteratogen. ..
  31. Mechanisms of Nicotine Induced Neurogenic Inflammation
    Kenneth Hargreaves; Fiscal Year: 2005
    ..nicotinic acetylcholine receptors (nAChRs) are capable of mediating antinociception in response to certain nicotinic agonists. We propose to test this hypothesis by addressing the following specific aims: 1) To quantify and ..
  32. NICOTINE ADDICTION IN MICE LACKING THE NEURONAL NACHR
    MARINA PICCIOTTO; Fiscal Year: 2004
    ..The specificity of existing nicotinic agonists for the different subtypes of the nAChR will be examined by comparing the binding of these agonists in the ..
  33. MECHANISMS OF CHLORPYRIFOS DEVELOPMENTAL NEUROTOXICITY
    Theodore Slotkin; Fiscal Year: 2004
    ..Molecular mechanisms of developmental neurotoxicity can be determined and linked to eventual alterations in behavioral performance. ..
  34. Fetal & Adolescent Nicotine Effects on CNS 5HT Systems
    Theodore Slotkin; Fiscal Year: 2003
    ..abstract_text> ..
  35. DRUGS AND DEVELOPMENT OF THE ADRENERGIC NERVOUS SYSTEM
    Theodore Slotkin; Fiscal Year: 2003
    ....
  36. Nicotine Vaccine & Nicotine Occupancy of Brain Nicotinic Receptors
    Irina Esterlis; Fiscal Year: 2010
    ..abstract_text> ..
  37. High Dose Nicotine Patch Therapy for Spit Tobacco Users
    Jon Ebbert; Fiscal Year: 2004
    ..Our goal is to reduce the prevalence of ST use and decrease the incidence of oropharyngeal cancer through the development of effective treatment options for ST users. ..
  38. Brief Dental Office Intervention with Tobacco Quitline
    Jon Ebbert; Fiscal Year: 2005
    ..S. adult population smoking; and 3) 75% of smokers quitting for at least one day or longer because they are trying to quit. ..
  39. Cocaine Withdrawal and Pharmacotherapy Response
    Mehmet Sofuoglu; Fiscal Year: 2010
    ..This proposal, by testing the efficacy of carvedilol and investigating the influence of withdrawal severity on carvedilol's efficacy, may result in development of more effective treatments for cocaine addiction. ..
  40. Evaluating Nicotine Lozenges for Treatment of Smokeless Tobacco Addiction
    Jon Ebbert; Fiscal Year: 2009
    ..No drug therapies have been shown to be effective for helping smokeless tobacco users quit for good. The purpose of this study is to test drugs that can be used to help smokeless tobacco users quit for good. ..
  41. Progestrone and the Effects of Nicotine
    Mehmet Sofuoglu; Fiscal Year: 2006
    ..By characterizing the progesterone effects on nicotine dependence, this study may provide a better understanding of the mechanisms which mediate the sex and menstrual cycle phase effects on nicotine dependence. ..
  42. GABA Medications for Tobacco Addiction
    Mehmet Sofuoglu; Fiscal Year: 2009
    ..The findings of this study will provide valuable information to develop new pharmacotherapies for smoking cessation. ..
  43. DISCRIMINATIVE STIMULUS EFFECTS OF NICOTINE
    Kenneth Perkins; Fiscal Year: 2001
    ....
  44. Tobacco Smoking, Nicotine and Negative Affect Relief
    Kenneth Perkins; Fiscal Year: 2009
    ..In sum, this research will help address the fundamental question of why cigarette smoking is reinforcing. ..
  45. SEX DIFFERENCES IN NICOTINE REINFORCEMENT: HUMAN/ANIMAL
    Kenneth Perkins; Fiscal Year: 2003
    ....
  46. Affect, Context, and Placebo Responses to Nicotine
    Kenneth Perkins; Fiscal Year: 2005
    ..Secondary analyses may identify important individual characteristics associated with placebo responses, aiding in the prediction of which smokers ultimately are likely to benefit most from manipulation of placebo effects. ..
  47. Internal Barriers to Seeking Smoking Cessation Treatment
    John Hughes; Fiscal Year: 2007
    ..Our results will suggest messages for media campaigns and for clinicians to use to motivate smokers to access proven treatments. ..
  48. INDIVIDUAL VARIATION IN NICOTINE SENSITIVITY IN HUMANS
    Kenneth Perkins; Fiscal Year: 2003
    ..e., in nicotine-naive individuals). Results will provide directions for future research on vulnerability to tobacco dependence and for targeted efforts to prevent smoking onset. ..
  49. Natural History of Attempts to Stop Smoking
    John R Hughes; Fiscal Year: 2010
    ....
  50. EVALUATION OF A CIGARETTE SUBSTITUTE
    John Hughes; Fiscal Year: 2001
    ..We believe it imperative to begin studying these substitutes so that, unlike low-tar/low nicotine cigarettes, we will know whether their introduction is good or bad for public health. ..
  51. Gradual vs Abrupt Cessation Treatment for Smoking
    John Hughes; Fiscal Year: 2007
    ..This study will be the first large, systematic test of gradual vs. abrupt cessation. ..
  52. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  53. Reference-dose method and cocaine-conditioned choice
    RICK BEVINS; Fiscal Year: 2006
    ..That research could translate into more effective intervention strategies. ..
  54. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Ivy Carroll; Fiscal Year: 2010
    ..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
  55. Acquired Appetitive Properties of Nicotine
    Rick A Bevins; Fiscal Year: 2010
    ....
  56. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
    ..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
  57. PAVLOVIAN CONDITIONING PROCESSES INVOLVING NICOTINE
    RICK BEVINS; Fiscal Year: 2001
    ..intermittent delivery). Elucidating the behavioral processes underlying acquisition and expression of Pavlovian drug conditioning will have important implications for prevention and intervention strategies. ..
  58. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  59. Smoking Cessation for Head and Neck Cancer Patients
    Robert Schnoll; Fiscal Year: 2006
    ..In turn, our findings may help guide the implementation of smoking cessation treatments for all cancer patients within Comprehensive Cancer Centers in the US. ..
  60. Interventions for Tobacco Dependent Adolescents
    Dorothy Hatsukami; Fiscal Year: 2005
    ....
  61. TREATMENT OF SMOKELESS TOBACCO USERS
    Dorothy Hatsukami; Fiscal Year: 2008
    ..PERFORMANCE SITE ========================================Section End=========================================== ..
  62. INSECTICIDE ACTIONS ON GABA-A RECEPTORS
    Gustav Akk; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  63. ROLE OF THE HIGH AFFINITY NICOTINE RECEPTOR IN ADDICTION
    MARINA PICCIOTTO; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable]..
  64. Actions of Ethanol on Ligand-Gated Ion Channels
    Gustav Akk; Fiscal Year: 2006
    ..The results from the experiments will be used to examine the mechanism and structural requirements in the ethanol-mediated modulation of the GABAA receptor function. ..
  65. Innovative Interventions for Smoking Cessation
    Dorothy K Hatsukami; Fiscal Year: 2010
    ..The results of this study will provide useful information on directions to pursue to improve our pharmacotherapies and behavioral treatments and to better understand the various aspects of addiction. ..