azocines

Summary

Top Publications

  1. ncbi Phytotoxicity of 2,4,6-trinitrotoluene (TNT) and octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine (HMX) in spiked artificial and natural forest soils
    P Y Robidoux
    Applied Ecotoxicology Group, Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2 Canada
    Arch Environ Contam Toxicol 44:198-209. 2003
  2. ncbi Toxicity and uptake of cyclic nitramine explosives in ryegrass Lolium perenne
    Sylvie Rocheleau
    Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec H4P 2R2, Canada
    Environ Pollut 156:199-206. 2008
  3. pmc Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
    H Rollema
    Neuroscience Biology, Groton, CT 06340, USA
    Br J Pharmacol 160:334-45. 2010
  4. 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
  5. ncbi Antidepressant effects of nicotine in an animal model of depression
    Y Tizabi
    Department of Pharmacology, College of Medicine, Howard University, Washington, DC 20059, USA
    Psychopharmacology (Berl) 142:193-9. 1999
  6. 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
  7. ncbi Cytisine for smoking cessation: a literature review and a meta-analysis
    Jean Francois Etter
    Institute of Social and Preventive Medicine, University of Geneva, 1 rue Michel Servet, CH 1211 Geneva 4, Switzerland
    Arch Intern Med 166:1553-9. 2006
  8. ncbi Fatal cytisine intoxication and analysis of biological samples with LC-MS/MS
    F Musshoff
    Institute of Forensic Medicine, Stiftsplatz 12, 53111 Bonn, Germany
    Forensic Sci Int 186:e1-4. 2009
  9. ncbi Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes
    Eric Carbonnelle
    CNR, Institute of Neuroscience, Section of Cellular and Molecular Pharmacology, Department of Medical Pharmacology and Center of Excellence on Neurodegenerative Diseases, University of Milan, Via Vanvitelli 32, 20129 Milan, Italy
    Eur J Pharmacol 471:85-96. 2003
  10. ncbi Cytisine's potential to be used as a traditional healing method to help indigenous people stop smoking: a qualitative study with Māori
    Te Pora Thompson-Evans
    Centre for Tobacco Control Research, Social and Community Health, School of Population Health, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand
    Nicotine Tob Res 13:353-60. 2011

Detail Information

Publications158 found, 100 shown here

  1. ncbi Phytotoxicity of 2,4,6-trinitrotoluene (TNT) and octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine (HMX) in spiked artificial and natural forest soils
    P Y Robidoux
    Applied Ecotoxicology Group, Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2 Canada
    Arch Environ Contam Toxicol 44:198-209. 2003
    ..4% at 91.4 +/- 7.9 mg/kg initial concentration, respectively. Data indicate that TNT is the probable phytotoxicant because it decreased plant emergence and growth in the presence and absence of the ADNT metabolites...
  2. ncbi Toxicity and uptake of cyclic nitramine explosives in ryegrass Lolium perenne
    Sylvie Rocheleau
    Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec H4P 2R2, Canada
    Environ Pollut 156:199-206. 2008
    ..These studies showed that RDX, HMX, and CL-20 can accumulate in plants and may potentially pose a risk of biomagnification across the food chain...
  3. pmc Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
    H Rollema
    Neuroscience Biology, Groton, CT 06340, USA
    Br J Pharmacol 160:334-45. 2010
    ..This work examines the origin of the differences by taking into account brain exposure and pharmacological effects at human alpha4beta2 nAChRs...
  4. 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...
  5. ncbi Antidepressant effects of nicotine in an animal model of depression
    Y Tizabi
    Department of Pharmacology, College of Medicine, Howard University, Washington, DC 20059, USA
    Psychopharmacology (Berl) 142:193-9. 1999
    ..These data strongly implicate the involvement of central nicotinic receptors in the depressive characteristics of the FSL rats, and suggest that nicotinic agonists may have therapeutic benefits in depressive disorders...
  6. 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...
  7. ncbi Cytisine for smoking cessation: a literature review and a meta-analysis
    Jean Francois Etter
    Institute of Social and Preventive Medicine, University of Geneva, 1 rue Michel Servet, CH 1211 Geneva 4, Switzerland
    Arch Intern Med 166:1553-9. 2006
    ..Cytisine has been used to treat tobacco dependence for 40 years in Eastern Europe. The objective of this study was to review the literature on the effect of cytisine on smoking cessation...
  8. ncbi Fatal cytisine intoxication and analysis of biological samples with LC-MS/MS
    F Musshoff
    Institute of Forensic Medicine, Stiftsplatz 12, 53111 Bonn, Germany
    Forensic Sci Int 186:e1-4. 2009
    ..By exclusion of other causes of death an intoxication was determined as the cause of death with respiratory failure as the pathophysiological mechanism...
  9. ncbi Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes
    Eric Carbonnelle
    CNR, Institute of Neuroscience, Section of Cellular and Molecular Pharmacology, Department of Medical Pharmacology and Center of Excellence on Neurodegenerative Diseases, University of Milan, Via Vanvitelli 32, 20129 Milan, Italy
    Eur J Pharmacol 471:85-96. 2003
    ..Adding chemical groups of a different class or size to the basic nitrogen of cytisine leads to compounds that lose full agonist activity on the alpha 3 beta 4 and alpha 7 subtypes...
  10. ncbi Cytisine's potential to be used as a traditional healing method to help indigenous people stop smoking: a qualitative study with Māori
    Te Pora Thompson-Evans
    Centre for Tobacco Control Research, Social and Community Health, School of Population Health, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand
    Nicotine Tob Res 13:353-60. 2011
    ..This study aimed to explore cytisine's potential as a 'rongoā Māori' (traditional Māori remedy) and its attractiveness to Māori smokers compared with other cessation products...
  11. ncbi Halogenated cytisine derivatives as agonists at human neuronal nicotinic acetylcholine receptor subtypes
    Y E Slater
    School of Biological and Molecular Sciences, Oxford Brookes University, Gipsy Lane Campus, Oxford OX3 0BP, UK
    Neuropharmacology 44:503-15. 2003
    ....
  12. pmc Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity
    Sheela K Chellappan
    Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Illinois 60612, USA
    J Med Chem 49:2673-6. 2006
    ..The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine...
  13. ncbi Chemical medicine: novel 10-substituted cytisine derivatives with increased selectivity for alpha4beta2 nicotinic acetylcholine receptors
    Alan P Kozikowski
    Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, USA
    ChemMedChem 2:1157-61. 2007
  14. pmc Cytisine-based nicotinic partial agonists as novel antidepressant compounds
    Yann S Mineur
    Department of Psychiatry, Yale School of Medicine, New Haven, CT 06508, USA
    J Pharmacol Exp Ther 329:377-86. 2009
    ..These results suggest that novel nicotinic partial agonists may provide new possibilities for development of drugs to treat mood disorders...
  15. ncbi In silico characterization of cytisinoids docked into an acetylcholine binding protein
    Juan Andrés Abin-Carriquiry
    Department of Neurochemistry, Instituto de Investigaciones Biologicas Clemente Estable, Montevideo, Uruguay
    Bioorg Med Chem Lett 20:3683-7. 2010
    ..Our docking results also suggest that further structural modifications of these cytisinoids will not greatly alter their alpha4beta2*/alpha7 selectivity...
  16. ncbi Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes
    Bruno Tasso
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Genova, Viale Benedetto XV 3, 16139 Genova, Italy
    J Med Chem 52:4345-57. 2009
    ....
  17. ncbi Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands
    P Imming
    Department of Pharmaceutical Chemistry, Philipps-University, Marbacher Weg 6, D-35032 Marburg, Germany
    Eur J Med Chem 36:375-88. 2001
    ....
  18. ncbi Smoking during early pregnancy affects the expression pattern of both nicotinic and muscarinic acetylcholine receptors in human first trimester brainstem and cerebellum
    L Falk
    Karolinska Institutet, Neurotec Department, Division of Molecular Neuropharmacology, Karolinska University Hospital Huddinge, S 141 86, Stockholm, Sweden
    Neuroscience 132:389-97. 2005
    ..The findings indicate that early prenatal nicotine exposure affects the normal developmental pattern of the cholinergic system in human fetal brain...
  19. ncbi Cholinergic drugs potentiate human nicotinic alpha4beta2 acetylcholine receptors by a competitive mechanism
    Chantal J G M Smulders
    Institute for Risk Assessment Sciences, Utrecht University, P O Box 80176, NL 3508 TD Utrecht, The Netherlands
    Eur J Pharmacol 509:97-108. 2005
    ....
  20. ncbi Evidence for functional nicotinic receptors on pancreatic beta cells
    Hiroyasu Yoshikawa
    Endocrine Section, Department of Medicine, Norwegian University of Science and Technology, Trondheim N 7489, Norway
    Metabolism 54:247-54. 2005
    ..05. Our data indicate that functional nicotinic receptors are present in pancreatic islets and beta cells...
  21. ncbi Conformational mobility of immobilized alpha3beta2, alpha3beta4, alpha4beta2, and alpha4beta4 nicotinic acetylcholine receptors
    Ruin Moaddel
    Gerontology Research Center, National Institutes in Aging, National Institutes of Health, Baltimore, MD 21224 6825, USA
    Anal Chem 77:895-901. 2005
    ..The columns provide a unique ability to study the interactions of NCIs with both of these conformational states...
  22. ncbi Nicotine activation of alpha4* receptors: sufficient for reward, tolerance, and sensitization
    Andrew R Tapper
    Division of Biology, California Institute of Technology, Pasadena, CA 91125, USA
    Science 306:1029-32. 2004
    ..These data indicate that activation of a4* receptors is sufficient for nicotine-induced reward, tolerance, and sensitization...
  23. ncbi Nicotinic receptors regulate the release of glycine onto lamina X neurones of the rat spinal cord
    A Bradaia
    Laboratoire de Neurophysiologie Cellulaire et Intégrée, UMR 7519 CNRS ULP, 21 rue R Descartes, 67084 Strasbourg Cedex, France
    Neuropharmacology 43:1044-54. 2002
    ..These data demonstrate that neurones surrounding the central canal of the spinal cord present a glycinergic synaptic transmission which is modulated by terminal nAChRs...
  24. ncbi Maternal exposure to nicotine and chlorpyrifos, alone and in combination, leads to persistently elevated expression of glial fibrillary acidic protein in the cerebellum of the offspring in late puberty
    Ali Abdel-Rahman
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA
    Arch Toxicol 78:467-76. 2004
    ..Also, nicotine caused a decrease in the surviving neurons and an increased expression of GFAP in cerebellar white matter of the offspring on PND 60. These changes can lead to long-term neurological adverse health effects later in life...
  25. ncbi Pharmacological characterization of dopamine, norepinephrine and serotonin release in the rat prefrontal cortex by neuronal nicotinic acetylcholine receptor agonists
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 990:203-8. 2003
    ..The differences between nicotinic agonist induced catecholamine and serotonin release suggest involvement of distinct nAChRs...
  26. ncbi Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors
    Richard W Fitch
    Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892, USA
    Bioorg Med Chem Lett 15:1221-4. 2005
    ..Caulophylline methiodide was less potent than cytisine, but retained significant activity. Thiocytisine was relatively weak in potency and efficacy, but was significantly selective for the alpha4beta2 subtype...
  27. ncbi Modulation of inhibitory synaptic activity by a non-alpha4beta2, non-alpha7 subtype of nicotinic receptors in the substantia gelatinosa of adult rat spinal cord
    Daisuke Takeda
    Department of Oral Surgery, College of Dentistry, University of Florida, 1600 SW Archer Road, Gainesville, FL 32610, USA
    Pain 101:13-23. 2003
    ....
  28. ncbi Localization of [3H]nicotine, [3H]cytisine, [3H]epibatidine, and [125I]alpha-bungarotoxin binding sites in the brain of Macaca mulatta
    Zhi yan Han
    CNRS URA 2182 Récepteurs et Cognition, Institut Pasteur, 75724 Paris Cedex 15, France
    J Comp Neurol 461:49-60. 2003
    ..The distribution of the binding sites for alpha-bungarotoxin is larger in the brain of rhesus monkeys than in rodent brain, suggesting a more important role of alpha7 receptors in primates...
  29. ncbi The subunit composition and pharmacology of alpha-Conotoxin MII-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay
    Outi Salminen
    Institute for Behavioral Genetics, University of Colorado, Boulder, 80309, USA
    Neuropharmacology 48:696-705. 2005
    ....
  30. ncbi Ablation of primary afferent terminals reduces nicotinic receptor expression and the nociceptive responses to nicotinic agonists in the spinal cord
    Imran M Khan
    Department of Pharmacology, University of California, San Diego, CA 92093 0636, USA
    J Neurocytol 33:543-56. 2004
    ..Conversely, spinal nicotinic receptors not located on C-fibers play a primary role in the spinal pathways evoking spinally coordinated autonomic cardiovascular responses...
  31. ncbi In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine
    Jotham W Coe
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 15:2974-9. 2005
    ..In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine...
  32. ncbi Elimination of rat spinal substance P receptor bearing neurons dissociates cardiovascular and nocifensive responses to nicotinic agonists
    Imran M Khan
    Department of Pharmacology, University of California, San Diego, CA 92093 0636, USA
    Neuropharmacology 54:269-79. 2008
    ..Further, the exaggerated cardiovascular responses to cytisine following loss of NK1-r bearing cells suggest the presence of a nicotinic receptor-mediated stimulation of inhibitory circuits at the spinal level...
  33. ncbi Postnatal upregulation of alpha4 and alpha3 nicotinic receptor subunits in the brain of alpha7 nicotinic receptor-deficient mice
    W F Yu
    Karolinska Institutet, Department of Neurobiology, Care Sciences and Society, Division of Molecular Neuropharmacology, Karolinska University Hospital Huddinge, S 141 86 Stockholm, Sweden
    Neuroscience 146:1618-28. 2007
    ..These data suggest that increased levels of alpha4, alpha3-containing nAChRs, co-assembled with the alpha5 nAChR subunit, may contribute to the normal brain development of alpha7 -/- and alpha7 +/- mice...
  34. pmc Catecholamine outflow from mouse and rat brain slice preparations evoked by nicotinic acetylcholine receptor activation and electrical field stimulation
    P Scholze
    Center for Brain Research, Medical University of Vienna, Vienna, Austria
    Br J Pharmacol 151:414-22. 2007
    ..We have now used brain slices to investigate nicotine-induced catecholamine outflow in wild type (WT) and nAChR (beta2 and alpha5) knockout mice for a comparison with rat brain slice preparations...
  35. ncbi Genetic approaches identify differential roles for alpha4beta2* nicotinic receptors in acute models of antinociception in mice
    M I Damaj
    Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Box 980613, Richmond, VA 23298 0613, USA
    J Pharmacol Exp Ther 321:1161-9. 2007
    ....
  36. ncbi Characterization of nicotinic acetylcholine receptors that modulate nicotine-evoked [3H]norepinephrine release from mouse hippocampal synaptosomes
    Layla Azam
    Department of Biology, University of Utah, 257 S 1400 E, Salt Lake City, UT 84112, USA
    Mol Pharmacol 70:967-76. 2006
    ..The sum of these results suggests a possible novel nAChR subtype that modulates nor-adrenergic neurotransmission within the mouse hippocampus...
  37. ncbi Deletion of the alpha7, beta2, or beta4 nicotinic receptor subunit genes identifies highly expressed subtypes with relatively low affinity for [3H]epibatidine
    Michael J Marks
    Institute for Behavioral Genetics, 447 UCB, University of Colorado, Boulder, CO 80309, USA
    Mol Pharmacol 70:947-59. 2006
    ....
  38. ncbi Prenatal nicotine exposure alters the nicotinic receptor subtypes that modulate excitation of parasympathetic cardiac neurons in the nucleus ambiguus from primarily alpha3beta2 and/or alpha6betaX to alpha3beta4
    Harriet Kamendi
    Department of Pharmacology and Physiology, George Washington University, 2300 Eye Street, N W Washington, DC 20037, USA
    Neuropharmacology 51:60-6. 2006
    ..These data demonstrate that the prenatal nicotine exposure alters the nicotinic receptors involved in excitation of cardiac vagal neurons...
  39. ncbi C3-halogenation of cytisine generates potent and efficacious nicotinic receptor agonists
    J Andrés Abin-Carriquiry
    IIBCE, Montevideo, Uruguay
    Eur J Pharmacol 536:1-11. 2006
    ..These compounds were also more efficacious than cytisine. C3-halogenation of cytisine is proposed to stabilize the open conformation of the nicotinic receptor but does not enhance subtype selectivity...
  40. ncbi From ligand design to therapeutic efficacy: the challenge for nicotinic receptor research
    Bruce K Cassels
    Department of Chemistry, Faculty of Sciences, University of Chile, Casilla 653, Santiago, Chile
    Drug Discov Today 10:1657-65. 2005
    ..Here, we focus on three natural products as lead compounds for drug discovery programs, nicotine, epibatidine and cytisine, and consider the aims and limitations that shape these drug discovery endeavors...
  41. ncbi Mouse beta-TC6 insulinoma cells: high expression of functional alpha3beta4 nicotinic receptors mediating membrane potential, intracellular calcium, and insulin release
    Masahiro Ohtani
    Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892 0820, USA
    Mol Pharmacol 69:899-907. 2006
    ..The binding and functional data suggest that the major nicotinic receptor is composed of alpha3 and beta4 subunits. The beta-TC6 cells thus provide a model system for pharmacological study of such nicotinic receptors...
  42. pmc Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells
    Loredana Riganti
    CNR, Institute of Neuroscience, Cellular and Molecular Pharmacology, Department of Medical Pharmacology and Center of Excellence on Neurodegenerative Diseases, University of Milan, Via Vanvitelli 32, 20129 Milan, Italy
    Br J Pharmacol 146:1096-109. 2005
    ....
  43. ncbi Subtypes of neuronal nicotinic acetylcholine receptors involved in nicotine-induced phosphorylation of extracellular signal-regulated protein kinase in PC12h cells
    Hitoshi Nakayama
    Department of Pharmacology, Nara Medical University School of Medicine, 840 Shijo Chou, Kashihara, Japan
    Neurosci Lett 392:101-4. 2006
    ..These results suggest the involvement of alpha3beta4 nAChRs in ERK phosphorylation in PC12h cells...
  44. ncbi A robust homogeneous binding assay for alpha4beta2 nicotinic acetylcholine receptor
    Xin Hui
    The National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Graduate School of Chinese Academy of Sciences, Shanghai 201203, China
    Acta Pharmacol Sin 26:1175-80. 2005
    ..To develop a homogeneous high-throughput screening (HTS) assay based on scintillation proximity assay (SPA) technology for identification of novel alpha4beta2 nicotinic acetylcholine receptor (nAChR) modulators...
  45. ncbi Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus: a function mediated by a different nAChR than dopamine release from striatum
    S R Grady
    Institute for Behavioral Genetics, University of Colorado, Boulder, Colorado 80309-0447, USA
    J Neurochem 76:258-68. 2001
    ....
  46. pmc Functional properties of human nicotinic AChRs expressed by IMR-32 neuroblastoma cells resemble those of alpha3beta4 AChRs expressed in permanently transfected HEK cells
    M E Nelson
    Department of Neuroscience, University of Pennsylvania Medical School, Philadelphia, PA 19104, USA
    J Gen Physiol 118:563-82. 2001
    ..These data show that even with the potential to express several human nicotinic AChR subtypes, the functional properties of AChRs expressed by IMR-32 are completely attributable to alpha3beta4 AChRs...
  47. ncbi Effect of nicotine on cerebellar granule neuron development
    L A Opanashuk
    Department of Anatomy and Neurobiology, University of Kentucky College of Medicine, Lexington, Kentucky 40536-0298, USA
    Eur J Neurosci 13:48-56. 2001
    ..Together these data provide novel evidence that the activation of nAChRs directly affect the development of primary cerebellar neuroblasts and further suggest that the effects are mediated through the alpha3-nAChR subtype...
  48. pmc Autonomic function in mice lacking alpha5 neuronal nicotinic acetylcholine receptor subunit
    Ningshan Wang
    Department of Physiology and Pharmacology, Sackler Medical School, Tel Aviv University, Israel
    J Physiol 542:347-54. 2002
    ..Thus, the data presented here imply that alpha5 subunits modulate the activity of nAChR in autonomic ganglia in vivo...
  49. ncbi Differential nicotinic receptor expression in monkey basal ganglia: effects of nigrostriatal damage
    M Quik
    The Parkinson s Institute, Sunnyvale, CA 94089, USA
    Neuroscience 112:619-30. 2002
    ..However, nicotinic receptor ligands with a broader specificity may be more important if receptors in the substantia nigra play a dominant role in controlling nigrostriatal activity...
  50. ncbi Regional distribution of nicotinic receptors during prenatal development of human brain and spinal cord
    E Hellström-Lindahl
    Department of Clinical Neuroscience and Family Medicine, Karolinska Institutet, Huddinge University Hospital, Sweden
    Brain Res Dev Brain Res 108:147-60. 1998
    ..The early presence of nAChR proteins and gene transcripts shown in the present study suggests an important role for nAChRs in modulating dendritic outgrowth, establishment of neuronal connections and synaptogenesis during development...
  51. ncbi Pharmacological evaluation of a Br-76 analog of epibatidine: a potent ligand for studying brain nicotinic acetylcholine receptors
    Michael Kassiou
    Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown NSW 2050 Australia
    Synapse 45:95-104. 2002
    ..These preliminary results suggest that [(76)Br]BrPH has the potential to be a useful radioligand for studying the pharmacology of nicotinic acetylcholine receptors in preclinical experiments...
  52. ncbi Characterization of [(125) I]epibatidine binding and nicotinic agonist-mediated (86) Rb(+) efflux in interpeduncular nucleus and inferior colliculus of beta2 null mutant mice
    Michael J Marks
    Institute for Behavioral Genetics, University of Colorado, Boulder, Colorado, USA
    J Neurochem 81:1102-15. 2002
    ..Thus, beta2 null mutant mice express residual nicotinic activity with properties resembling those of alpha3beta4*-nAChR...
  53. ncbi Dorsal root ganglion neurons express multiple nicotinic acetylcholine receptor subtypes
    J R Genzen
    Committee on Neurobiology, University of Chicago, Chicago, Illinois 60637, USA
    J Neurophysiol 86:1773-82. 2001
    ..Both the alpha7-like and alpha3beta4-like responses could be desensitized by prolonged applications of the analgesic epibatidine...
  54. ncbi Differential regulation of nicotinic receptor-mediated neurotransmitter release following chronic (-)-nicotine administration
    Iris Jacobs
    Abbott Laboratories, Department 47W, Abbott Park Building AP 9A, Abbott Park, IL 60064 6125, USA
    Neuropharmacology 43:847-56. 2002
    ..These results support findings from earlier studies comparing the pharmacology of nAChR-evoked striatal versus cortical [(3)H]-DA release...
  55. ncbi A non-alpha7 nicotinic acetylcholine receptor modulates excitatory input to hippocampal CA1 interneurons
    Manickavasagom Alkondon
    Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, 655 W Baltimore Street, Baltimore, MD 21201, USA
    J Neurophysiol 87:1651-4. 2002
    ..We conclude that nAChR-dependent EPSC modulation in the hippocampus is both subtype- and neuron-specific and that a non-alpha7 nAChR, presumably alpha3beta4, controls glutamate transmission to CA1 interneurons...
  56. ncbi Nicotinic receptor gene cluster on rat chromosome 8 in nociceptive and blood pressure hyperresponsiveness
    Imran M Khan
    Department of Pharmacology, University of California, San Diego, California 92093 0636, USA
    Physiol Genomics 11:65-72. 2002
    ....
  57. ncbi Distribution and pharmacology of alpha 6-containing nicotinic acetylcholine receptors analyzed with mutant mice
    Nicolas Champtiaux
    Laboratoire de Neurobiologie Moléculaire, Centre National de la Recherche Scientifique, Unité de Recherche Associée 2182, Recepteurs et Cognition, Institut Pasteur 75724 Paris, Cedex 15, France
    J Neurosci 22:1208-17. 2002
    ..They further show that alpha6-/- mice might be useful tools to understand the mechanisms of nicotine addiction, although some developmental compensation might occur in these mice...
  58. ncbi Pharmacological characterization of nicotinic receptor-mediated acetylcholine release in rat brain--an in vivo microdialysis study
    Y Tani
    Suntory Institute for Biomedical Research, Osaka, Japan
    Eur J Pharmacol 351:181-8. 1998
    ....
  59. ncbi Antagonism of the analgesic effects of mu and kappa opioid agonists in the squirrel monkey
    L A Dykstra
    Department of Psychology, University of North Carolina, Chapel Hill
    J Pharmacol Exp Ther 246:813-21. 1988
    ..43 and 7.61, respectively; whereas the pA2 value for quadazocine in combination with bremazocine and U50,488 were 6.53 and 6.43, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)..
  60. pmc Monitoring cholinergic activity during attentional performance in mice heterozygous for the choline transporter: a model of cholinergic capacity limits
    Giovanna Paolone
    Department of Psychology and Neuroscience Program, University of Michigan, Ann Arbor, MI 48103, USA
    Neuropharmacology 75:274-85. 2013
    ..Further analyses of molecular and functional compensations in the CHT+/- model may provide insights into both risk and resiliency factors involved in cognitive and mood disorders. ..
  61. ncbi Physico-chemical measurements of CL-20 for environmental applications. Comparison with RDX and HMX
    Fanny Monteil-Rivera
    Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Que, H4P 2R2 Canada
    J Chromatogr A 1025:125-32. 2004
    ..N2O (2 equiv.), and HCOO- (2 equiv.). The experimental findings suggest that CL-20 should be less persistent in the environment than RDX and HMX...
  62. ncbi Bioremediation of nitroexplosive wastewater by an yeast isolate Pichia sydowiorum MCM Y-3 in fixed film bioreactor
    S P Kanekar
    Microbial Sciences Division, Agharkar Research Institute, G G Agarkar Road, Pune, 411004, Maharashtra, India
    J Ind Microbiol Biotechnol 36:253-60. 2009
    ..Thus, FFBR developed with baffles and operated in continuous mode will be beneficial for bioremediation of high nitrate and acetate containing wastewater using the culture of P. sydowiorum...
  63. ncbi Kappa opioid agonists inhibit transmitter release from guinea pig hippocampal mossy fiber synaptosomes
    R L Gannon
    Department of Anatomy and Cell Biology, East Carolina University, School of Medicine, Greenville, NC 27858
    Neurochem Res 17:741-7. 1992
    ..These results suggest that kappa opioid agonists inhibit transmitter release from mossy fiber terminals through both kappa opioid and non-kappa opioid receptor mediated mechanisms...
  64. ncbi Nicotinic receptor partial agonists as novel compounds for the treatment of smoking cessation
    Piotr Tutka
    Medical University of Lublin, Department of Experimental and Clinical Pharmacology, Lublin, Poland
    Expert Opin Investig Drugs 17:1473-85. 2008
    ..Very encouraging results of early human trials and strong theoretical background for their use make the nAChRs partial agonists a promising alternative for currently available antismoking treatments...
  65. pmc The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats
    Patricia E Grebenstein
    Department of Psychology, University of Florida, Gainesville, FL 32611 2250, USA Electronic address
    Pharmacol Biochem Behav 110:192-200. 2013
    ..Increased appetite and weight gain after cessation are deterrents for quitting smoking. Pharmacotherapies that can reduce this weight gain in ex-smokers would be invaluable, and yet are not well studied in this context...
  66. ncbi Halide salts accelerate degradation of high explosives by zerovalent iron
    Jong Sung Kim
    Center for Environmental Toxicology and School of Natural Resources, University of Nebraska Lincoln, 362 Plant Sciences, Lincoln, NE 68583, USA
    Environ Pollut 147:634-41. 2007
    ..HMX was most difficult to remove using ZVI alone but ZVI remained effective after five HMX reseeding cycles when Br(-) was present in solution...
  67. ncbi Chronic nicotine and dizocilpine effects on nicotinic and NMDA glutamatergic receptor regulation: interactions with clozapine actions and attentional performance in rats
    Amir H Rezvani
    Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC 27710, USA
    Prog Neuropsychopharmacol Biol Psychiatry 32:1030-40. 2008
    ..In conclusion, the data suggest attentional impairments with clozapine alone and no modification of this effect with nicotine or dizocilpine. Moreover, cortical low affinity nicotinic receptors may have a role in attentional functions...
  68. pmc Activity of opioid ligands in cells expressing cloned mu opioid receptors
    Parham Gharagozlou
    Department of Pharmacology, Molecular Research Institute, Mountain View, CA 94043, USA
    BMC Pharmacol 3:1. 2003
    ..Efficacies and potencies of these ligands were determined relative to the endogenous ligand beta-endorphin and the common mu agonist, morphine...
  69. ncbi Toxicity of explosive compounds to the marine mussel, Mytilus galloprovincialis, in aqueous exposures
    Gunther Rosen
    Space and Naval Warfare Systems Center, Environmental Sciences and Applied Systems Branch, 53475 Strothe Road, San Diego, CA 92152, USA
    Ecotoxicol Environ Saf 68:228-36. 2007
    ..6 and 0.92microg g(-1) (86 and 3.1nmolg(-1)) ww were not associated with any toxicity for RDX and HMX, respectively...
  70. ncbi First-principles study of the four polymorphs of crystalline octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine
    Weihua Zhu
    Institute for Computation in Molecular and Materials Science and Department of Chemistry, Nanjing University of Science and Technology, Nanjing 210094, China
    J Phys Chem B 111:12715-22. 2007
    ....
  71. ncbi Food avoidance behavior to dietary octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine (HMX) exposure in the northern bobwhite (Colinusvirginianus)
    Mark S Johnson
    US Army Center for Health Promotion and Preventative Medicine, Health Effects Research Program, Aberdeen Proving Ground, Maryland 21010 5403, USA
    J Toxicol Environ Health A 68:1349-57. 2005
    ..These results suggest that HMX concentration is responsible for intense feed aversion behavior and thus not likely a factor that would appreciably contribute to risk for wild birds at military ranges...
  72. ncbi Abiotic transformation of high explosives by freshly precipitated iron minerals in aqueous FeII solutions
    Hardiljeet K Boparai
    School of Natural Resources, University of Nebraska Lincoln, Lincoln, NE 68583, USA
    Chemosphere 79:865-72. 2010
    ..These results illustrate the important role freshly precipitated Fe(II)/Fe(III) minerals in aqueous Fe(II) solutions play in the transformation of high explosives...
  73. pmc Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors
    Kasper Harpsøe
    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark
    J Biol Chem 288:2559-70. 2013
    ....
  74. ncbi Characterization of human alpha4beta2 neuronal nicotinic receptors stably expressed in SH-EP1 cells
    M A Pacheco
    Department of Pharmacology and Therapeutics University of South Florida College of Medicine, Tampa 33612-4799, USA
    Neurochem Res 26:683-93. 2001
    ..Results indicate that SH-EPI-halpha4beta2 cells may be a good model system to study regulation of human alpha4beta2 receptors, the most abundant nicotinic receptor subtype in brain...
  75. ncbi Solvent-enhanced diastereo- and regioselectivity in the Pd(II)-catalyzed synthesis of six- and eight-membered heterocycles via cis-aminopalladation
    Arpád Balázs
    Institute of Pharmaceutical Chemistry, University of Szeged, 6720 Szeged, Eotvos u 6, Hungary
    Chemistry 15:7376-81. 2009
    ..Additionally, a novel Pd(II)-mediated domino oxidation, oxidative amination reaction was discovered. Our experimental and theoretical findings suggest that the reactions proceed via a cis-aminopalladation mechanism...
  76. ncbi Effects of cytisine on hydroxyl radicals in vitro and MPTP-induced dopamine depletion in vivo
    B Ferger
    Institute of Pharmacology and Toxicology, Faculty of Pharmacy, University of Marburg, Germany
    Eur J Pharmacol 360:155-63. 1998
    ..Thus, cytisine may be useful for the treatment of Parkinson's Disease where the chelation of iron ions could prevent neuronal cell death...
  77. ncbi Phenotypic characterization of an alpha 4 neuronal nicotinic acetylcholine receptor subunit knock-out mouse
    S A Ross
    Neurosciences Group, Monash University Department of Medicine and Institute of Reproduction and Development, Monash Medical Centre, Clayton, Victoria, 3168, Australia
    J Neurosci 20:6431-41. 2000
    ..Furthermore, the response of Mt to nicotine administration suggests that persistent nicotine binding sites in the habenulo-interpeduncular system are sufficient to modulate motor activity in actively exploring mice...
  78. ncbi Optically active Ru(II) complexes with a chiral Tröger's base ligand and their interactions with DNA
    Nicolas Claessens
    Chimie Organique et Photochimie, Universite Libre de Bruxelles, CP 160 08, 50 Avenue F D Roosevelt, 1050 Bruxelles, Belgium
    J Inorg Biochem 101:987-96. 2007
    ..The affinity constant for the stereoisomer Delta-S-2 is 10(2) higher than that for Lambda-S-2 and rac-[Ru(phen)3]2+...
  79. ncbi Spinal nicotinic receptor activity in a genetic model of hypertension
    I M Khan
    Department of Pharmacology, University of California, San Diego 92093 0636, USA
    Clin Exp Hypertens 23:555-68. 2001
    ..Overall, our findings suggest that hyper-responsiveness in nociception and pressor activity to spinal cytisine in SHR may be pathogenetically associated, but not a consequence, of hypertension...
  80. ncbi Cytisine confers neuronal protection against excitotoxic injury by down-regulating GluN2B-containing NMDA receptors
    Yu Jiao Li
    Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi an, Shaanxi Province 710032, PR China
    Neurotoxicology 34:219-25. 2013
    ..These findings suggest that CYT protects cortical neurons, at least partially, by inhibiting the level of GluN2B-containing NMDA receptors and regulating Bcl-2 family...
  81. ncbi A Raney-cobalt-mediated tandem reductive cyclization route to the 1,5-methanoazocino[4,3-b]indole framework of the uleine and Strychnos alkaloids
    Tristan A Reekie
    Research School of Chemistry, Institute of Advanced Studies, The Australian National University, Canberra ACT 0200, Australia
    J Org Chem 77:10773-81. 2012
    ..These products embody the ABCD-ring system associated with the title alkaloids, and compound 11 can be converted, over four steps and in 33% yield, into congener 24 incorporating the ABCDE-ring system of the Strychnos alkaloids...
  82. ncbi Dissolution kinetics of sub-millimeter Composition B detonation residues: role of particle size and particle wetting
    Mark E Fuller
    Shaw Environmental, Inc, 17 Princess Road, Lawrenceville, NJ 08648, USA
    Chemosphere 88:591-7. 2012
    ..g., dry physical attrition vs. aqueous weathering) of Composition B residues should be considered when calculating mass transfer rates for fate and transport modeling...
  83. ncbi A readily-accessible (+)-sparteine surrogate
    Michael J Dearden
    Department of Chemistry, University of York, Heslington, York YO10 5DD, U K
    J Am Chem Soc 124:11870-1. 2002
    ....
  84. ncbi Prenatal nicotine exposure alters the response to nicotine administration in adolescence: effects on cholinergic systems during exposure and withdrawal
    Yael Abreu-Villaça
    Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA
    Neuropsychopharmacology 29:879-90. 2004
    ....
  85. ncbi PET Imaging of nicotinic acetylcholine receptors in baboons with 18F-AZAN, a radioligand with improved brain kinetics
    Hiroto Kuwabara
    Division of Nuclear Medicine, Department of Radiology, Johns Hopkins School of Medicine, Baltimore, Maryland 21287 0816, USA
    J Nucl Med 53:121-9. 2012
    ..2.1]heptane ((18)F-AZAN), our new radiolabeled antagonist of α4β2-nAChRs, that has high binding potential and rapid brain kinetics in baboons...
  86. ncbi Addition of cyclic ureas and 1-methyl-2-oxazolidone to pyridynes: a new approach to pyridodiazepines, pyridodiazocines, and pyridooxazepines
    Nozomi Saito
    Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo 060 0812, Japan
    Org Lett 15:386-9. 2013
    ..3,4-Pyridyne and 2,3-pyridyne were reacted with N,N-dimethylimidazolidone, N,N-dimethylpropylene urea, and 1-methyl-2-oxazolidone to give the corresponding pyridodiazepines, pyridodiazocines, and pyridooxazepines, respectively...
  87. ncbi Solid-phase extraction using hierarchical organosilicates for enhanced detection of nitroenergetic targets
    Brandy J Johnson
    Center for Bio Molecular Science and Engineering, Naval Research Laboratory, Washington, DC, USA
    J Environ Monit 13:1404-9. 2011
    ..The results presented here demonstrate the potential of this novel sorbent for application as a solid phase extraction material for the preconcentration of nitroenergetic targets from aqueous solutions...
  88. ncbi Genetic correlation between the free-choice oral consumption of nicotine and alcohol in C57BL/6JxC3H/HeJ F2 intercross mice
    Xiao C Li
    Department of Integrative Physiology, Institute for Behavioral Genetics, University of Colorado, Boulder, CO 80309, USA
    Behav Brain Res 157:79-90. 2005
    ....
  89. pmc Potentiation of evoked calcitonin gene-related peptide release from oral mucosa: a potential basis for the pro-inflammatory effects of nicotine
    Gregory O Dussor
    Department of Pharmacology, The University of Texas Health Science Center, San Antonio, TX, USA
    Eur J Neurosci 18:2515-26. 2003
    ..In the case of users of nicotine-containing tobacco products, this modulation could contribute to inflammatory processes within the oral cavity...
  90. ncbi An entry to the azocino[4,3-b]indole framework through a dehydrogenative activation of 1,2,3,4-tetrahydrocarbazoles mediated by DDQ: formal synthesis of (±)-uleine
    Süleyman Patir
    Department of Chemistry Education, Faculty of Education, Hacettepe University, 06800 Beytepe, Ankara, Turkey
    J Org Chem 76:335-8. 2011
    ..Furthermore, this cyclization reaction was successfully utilized in the formal total synthesis of (±)-uleine, an Aspidospermatan skeletal type alkaloid...
  91. ncbi Neuronal nicotinic receptor ligands modulate chronic nicotine-induced ethanol consumption in C57BL/6J mice
    Ravi K Sajja
    Department of Pharmaceutical Sciences, South Dakota State University, College of Pharmacy, Brookings, SD 57007, USA
    Pharmacol Biochem Behav 102:36-43. 2012
    ..DHβE (0.5 or 2.0 mg/kg) failed to suppress nicotine-induced ethanol intake across 2 h post injection. These results indicate that nAChRmediated signaling is critical in regulating nicotine-induced ethanol drinking behaviors...
  92. ncbi Varenicline and cytisine: two nicotinic acetylcholine receptor ligands reduce ethanol intake in University of Chile bibulous rats
    Ramón Sotomayor-Zárate
    Departamento de Fisiologia, Facultad de Ciencias, Universidad de Valparaiso, Av Gran Bretaña 1111, Playa Ancha, Valparaiso, Chile
    Psychopharmacology (Berl) 227:287-98. 2013
    ..Varenicline and cytisine are nAChR partial agonists in clinical use as smoking cessation aids. However, their efficacies to reduce alcohol consumption have not been fully studied...
  93. ncbi Nicotinic receptor partial agonists alter catecholamine homeostasis and response to nicotine in PC12 cells
    D S Turcanu
    Division of Newborn Medicine, Department of Pediatrics, New York Medical College, Valhalla, NY 10595, USA
    Neurosci Lett 516:212-6. 2012
    ..e. NE release and re-synthesis) and (ii) modulated the effect of nicotine during combined treatment...
  94. ncbi IBU-octyl-cytisine, a novel bifunctional compound eliciting anti-inflammatory and cholinergic activity, ameliorates CNS inflammation by inhibition of T-cell activity
    Eran Nizri
    Laboratory of Neuroimmunology, Department of Neurology and the Agnes Ginges Center for Human Neurogenetics, Hadassah Hebrew University Medical Center, Jerusalem, Israel
    Int Immunopharmacol 7:1129-39. 2007
    ..This bifunctional compound was more efficient than IBU or Cytisine separately, as well as than both moieties unconjugated. Thus, it seems that this strategy may be applicable in wider context...
  95. ncbi Cytotoxic and genotoxic effects of energetic compounds on bacterial and mammalian cells in vitro
    B Lachance
    Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec, Canada
    Mutat Res 444:25-39. 1999
    ..In view of earlier reports and this study, mutagenicity testing of environmental samples should be considered as part of the hazard assessment of sites contaminated by TNT and related products...
  96. ncbi Pharmacologic evaluation of isometric contraction-relaxation coupling indexes in rabbit ventricular muscle
    S Baudet
    Laboratoire de Physiopathologie et Pharmacologie Cellulaires et Moléculaires, CJF INSERM 96 01, Hotel Dieu, F 44093, Nantes Cedex, France
    J Pharmacol Toxicol Methods 42:21-30. 1999
    ....
  97. ncbi 7-Azaindole derivatives as potential partial nicotinic agonists
    Axel R Stoit
    Solvay Pharmaceuticals, Research Laboratories, C J van Houtenlaan 36, 1381 CP Weesp, The Netherlands
    Bioorg Med Chem Lett 18:188-93. 2008
    ..Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation...
  98. pmc Gene targeting demonstrates that alpha4 nicotinic acetylcholine receptor subunits contribute to expression of diverse [3H]epibatidine binding sites and components of biphasic 86Rb+ efflux with high and low sensitivity to stimulation by acetylcholine
    Michael J Marks
    Institute for Behavioral Genetics, 447 UCB, University of Colorado, Boulder, CO 80309, USA
    Neuropharmacology 53:390-405. 2007
    ..These effects are very similar to those following deletion of beta2. Thus, alpha4beta2*-nAChRs mediate a significant fraction of both phases of ACh stimulated 86Rb+ efflux...
  99. ncbi Contribution of hydrolysis in the abiotic attenuation of RDX and HMX in coastal waters
    Fanny Monteil-Rivera
    Biotechnology Research Institute, National Research Council of Canada, 6100 Royalmount Avenue, Montreal, Quebec, Canada
    J Environ Qual 37:858-64. 2008
    ..0%). We concluded that under natural conditions hydrolysis should not contribute significantly to the natural attenuation of HMX in coastal waters whereas it could play an active role in the natural attenuation of RDX...
  100. ncbi Identification of explosives with two-dimensional ultraviolet resonance Raman spectroscopy
    Gelu Comanescu
    Research Support Instruments, Lanham, Maryland 20706, USA
    Appl Spectrosc 62:833-9. 2008
    ..We have recently shown that 2D resonance Raman spectra can identify bacteria. Thus, a single device that identifies the presence of explosives, bacteria, and other chemicals in complex backgrounds may be feasible...
  101. ncbi An expedient and facile route for the general synthesis of 3-aryl substituted 1,2,3-triazolo[1,5-a][1,4]benzodiazepin-6-ones and 1,2,3-triazolo[1,5-a][1,5]benzodiazocin-7-ones
    Chinmay Chowdhury
    Chemistry Division, Indian Institute of Chemical Biology CSIR, 4, Raja S C Mullick Road, Kolkata, 700032, India
    Org Biomol Chem 8:4971-7. 2010
    ..The strategy also allows easy accessibility of the corresponding amide-reduced analogues. The operational simplicity and easy substrate availability make the process cost effective and practical...

Research Grants19

  1. 2,5 CYCLOHEXADIENONES IN NATURAL PRODUCTS SYNTHESIS
    Mark Wentland; Fiscal Year: 2001
    ....
  2. AMINOBENZOMORPHAN: POTENTIAL COCAINE ABUSE MEDICATIONS
    Mark Wentland; Fiscal Year: 2009
    ..Radioligand binding, [35S]GTPvS, and mouse antinociceptive assays will be used to characterize new targets pharmacologically. ..
  3. EAMG: MIR structure and specific immunosuppressive therapy
    Jon Lindstrom; Fiscal Year: 2009
    ..Our long term goal is to test an optimized therapy on canine MG as a model for human studies. ..
  4. BIOLOGICAL STUDIES OF PIPERIDINE ANALOGS OF COCAINE
    Alan Kozikowski; Fiscal Year: 2001
    ..4. For compounds meeting set criteria, to further evaluate their behavioral pharmacological profile in animals using intravenous drug self-administration and drug discrimination procedures. ..
  5. Evaluation in Primates of Cocaine Esterase for the Treatment of Cocaine Toxicity
    Mei Chuan Ko; Fiscal Year: 2010
    ..Dose-response functions for each enzyme will be obtained repeatedly and blood samples analyzed for titer development so that tolerance to the effects of CocE can be monitored. ..
  6. THE ROLE OF EPSILON SUBUNIT IN GABAA RECEPTOR FUNCTION
    David C Perry; Fiscal Year: 2010
    ..A better understanding of GABAA receptors and their potential for adaptation will help increase our understanding of changes in neuronal inhibition during epilepsy. ..
  7. Chemistry and Biology of 5-HT2C Receptor Ligands for Drug Abuse
    ALAN PAUL KOZIKOWSKI; Fiscal Year: 2010
    ....
  8. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2003
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  9. Fetal & Adolescent Nicotine Effects on CNS 5HT Systems
    Theodore Slotkin; Fiscal Year: 2003
    ..abstract_text> ..
  10. DESIGN OF LIGANDS SELECTIVE FOR THE DAG SUPERFAMILY
    Alan Kozikowski; Fiscal Year: 2002
    ..To assess the effect of alterations in the ligand's hydrophobic side chain on its tumor promoting activity, studies of skin hyperplasia will be conducted. ..
  11. PKC Modulators for the Treatment of Alzheimer's disease
    Alan Kozikowski; Fiscal Year: 2008
    ..For the best compounds from Aim 2, perform studies in triple transgenic mice to ascertain effects on Abeta and sAPPalpha levels and plaque formation in vivo. ..
  12. Chemistry and Pharmacology of a New Nicotine Ligands
    Alan Kozikowski; Fiscal Year: 2007
    ..Functional activity will be evaluated using established 86RbC1 efflux assays and/or whole cell patch clamp measurements. ..
  13. Characterization of nAChRs using novel alpha-conotoxins
    Layla Azam; Fiscal Year: 2005
    ..abstract_text> ..
  14. Improving the Wegner Hall Vivarium
    BRYAN SLINKER; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  15. CHEMICAL AND PHARMACOLOGICAL STUDIES OF COCAINE ANALOGS
    Alan Kozikowski; Fiscal Year: 2004
    ....
  16. 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. ..
  17. DRUGS AND DEVELOPMENT OF THE ADRENERGIC NERVOUS SYSTEM
    Theodore Slotkin; Fiscal Year: 2003
    ....
  18. GABAergic excitation in human hypothalamic hamartoma
    Jie Wu; Fiscal Year: 2007
    ..Knowledge about excitatory GABAA receptor function of HH neurons will also aid selection of superior strategies for pharmaceutical development to prevent and control human gelastic seizures. [unreadable] [unreadable]..