isoxazoles

Summary

Summary: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.

Top Publications

  1. ncbi 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer
    Paul A Brough
    Vernalis Ltd, Granta Park, Great Abington, Cambridge CB21 6GB, U K p brough vernalis com
    J Med Chem 51:196-218. 2008
  2. ncbi Synthesis and antitumor activity of 2,5-bis(3'-indolyl)-furans and 3,5-bis(3'-indolyl)-isoxazoles, nortopsentin analogues
    Patrizia Diana
    Dipartimento Farmacochimico, Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Bioorg Med Chem 18:4524-9. 2010
  3. ncbi Safety and tolerability of deltoid and gluteal injections of paliperidone palmitate in schizophrenia
    David Hough
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ, USA
    Prog Neuropsychopharmacol Biol Psychiatry 33:1022-31. 2009
  4. ncbi Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma
    T Stühmer
    Department of Internal Medicine II, Division of Hematology, University Hospital Wurzburg, Wurzburg, Germany
    Leukemia 22:1604-12. 2008
  5. pmc Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site
    Gareth T Young
    Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, United Kingdom
    Proc Natl Acad Sci U S A 105:14686-91. 2008
  6. ncbi Paliperidone palmitate maintenance treatment in delaying the time-to-relapse in patients with schizophrenia: a randomized, double-blind, placebo-controlled study
    David Hough
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, New Jersey, USA
    Schizophr Res 116:107-17. 2010
  7. ncbi Plasma and CNS concentrations of Gaboxadol in rats following subcutaneous administration
    Thomas Cremers
    Brains on Line, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands
    Eur J Pharmacol 562:47-52. 2007
  8. pmc AHR2 mutant reveals functional diversity of aryl hydrocarbon receptors in zebrafish
    Britton C Goodale
    Department of Environmental and Molecular Toxicology, Environmental Health Sciences Center, Oregon State University, Corvallis, Oregon, United States of America
    PLoS ONE 7:e29346. 2012
  9. ncbi Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation
    Laura del Barrio
    Instituto Teofilo Hernando, Facultad de Medicina, Universidad Auto noma de Madrid, 28029 Madrid, Spain
    Toxicol Sci 123:193-205. 2011
  10. ncbi Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem
    Tim R M Leufkens
    Experimental Psychopharmacology Unit, Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands
    J Sleep Res 18:387-96. 2009

Detail Information

Publications282 found, 100 shown here

  1. ncbi 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer
    Paul A Brough
    Vernalis Ltd, Granta Park, Great Abington, Cambridge CB21 6GB, U K p brough vernalis com
    J Med Chem 51:196-218. 2008
    ..Compound 40f is retained in tumors in vivo when administered i.p., as evaluated by cassette dosing in tumor-bearing mice. In a human colon cancer xenograft model, 40f inhibits tumor growth by approximately 50%...
  2. ncbi Synthesis and antitumor activity of 2,5-bis(3'-indolyl)-furans and 3,5-bis(3'-indolyl)-isoxazoles, nortopsentin analogues
    Patrizia Diana
    Dipartimento Farmacochimico, Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Bioorg Med Chem 18:4524-9. 2010
    A series of novel 2,5-bis(3'-indolyl)furans and 3,5-bis(3'-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines...
  3. ncbi Safety and tolerability of deltoid and gluteal injections of paliperidone palmitate in schizophrenia
    David Hough
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ, USA
    Prog Neuropsychopharmacol Biol Psychiatry 33:1022-31. 2009
    ..Paliperidone palmitate treatment was tolerated, irrespective of injection site, and thus could offer the choice of administration into either the deltoid or gluteal muscle to meet patient and physician preference...
  4. ncbi Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma
    T Stühmer
    Department of Internal Medicine II, Division of Hematology, University Hospital Wurzburg, Wurzburg, Germany
    Leukemia 22:1604-12. 2008
    ..Thus, NVP-AUY922 may be a promising drug for treatment of MM and clinical studies are warranted...
  5. pmc Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site
    Gareth T Young
    Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, United Kingdom
    Proc Natl Acad Sci U S A 105:14686-91. 2008
    ..Our findings suggest that this is a conserved modulatory allosteric site within neurotransmitter-gated ion channels...
  6. ncbi Paliperidone palmitate maintenance treatment in delaying the time-to-relapse in patients with schizophrenia: a randomized, double-blind, placebo-controlled study
    David Hough
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, New Jersey, USA
    Schizophr Res 116:107-17. 2010
    ..We assessed efficacy and tolerability of the injectable atypical antipsychotic paliperidone palmitate in delaying time-to-relapse in adults with schizophrenia...
  7. ncbi Plasma and CNS concentrations of Gaboxadol in rats following subcutaneous administration
    Thomas Cremers
    Brains on Line, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands
    Eur J Pharmacol 562:47-52. 2007
    ..It is concluded that concentrations of Gaboxadol in the CNS are in a range, which are likely to activate only extrasynaptic (nongamma subunit containing) GABA(A) receptors...
  8. pmc AHR2 mutant reveals functional diversity of aryl hydrocarbon receptors in zebrafish
    Britton C Goodale
    Department of Environmental and Molecular Toxicology, Environmental Health Sciences Center, Oregon State University, Corvallis, Oregon, United States of America
    PLoS ONE 7:e29346. 2012
    ....
  9. ncbi Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation
    Laura del Barrio
    Instituto Teofilo Hernando, Facultad de Medicina, Universidad Auto noma de Madrid, 28029 Madrid, Spain
    Toxicol Sci 123:193-205. 2011
    ..Therefore, targeting nAChR could offer a strategy for reducing neurodegeneration secondary to hyperphosphorylation of protein τ...
  10. ncbi Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem
    Tim R M Leufkens
    Experimental Psychopharmacology Unit, Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands
    J Sleep Res 18:387-96. 2009
    ..Administration later at night is associated with moderately impairing residual effects on driving and psychomotor performance but not on memory...
  11. ncbi Whole genome association study identifies polymorphisms associated with QT prolongation during iloperidone treatment of schizophrenia
    S Volpi
    Vanda Pharmaceuticals Inc, Rockville, MD 20850, USA
    Mol Psychiatry 14:1024-31. 2009
    ..Results of this pharmacogenomic study provide new insight into the clinical response to iloperidone, developed with the goal of directing therapy to those patients with the optimal benefit/risk ratio...
  12. ncbi The immunomodulatory drug Leflunomide inhibits cell cycle progression of B-CLL cells
    I Ringshausen
    Leukemia 22:635-8. 2008
  13. ncbi Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia
    John M Kane
    Department of Psychiatry, The Zucker Hillside Hospital, Glen Oaks, NY 11004, USA
    J Clin Psychopharmacol 28:S29-35. 2008
    ..4 msec (haloperidol) at end point. Iloperidone demonstrated long-term efficacy equivalent to haloperidol and a favorable long-term safety profile, potentially making this agent a suitable option as maintenance therapy for schizophrenia...
  14. pmc Teriflunomide (leflunomide) promotes cytostatic, antioxidant, and apoptotic effects in transformed prostate epithelial cells: evidence supporting a role for teriflunomide in prostate cancer chemoprevention
    Numsen Hail
    Department of Pharmaceutical Sciences, University of Colorado Denver School of Pharmacy, 12700 E 19th Avenue, Aurora, CO 80045, USA
    Neoplasia 12:464-75. 2010
    ..These mechanistic findings advocate a role for TFN and mitochondrial bioenergetics in prostate cancer chemoprevention...
  15. ncbi Critical role of macrophage migration inhibitory factor activity in experimental autoimmune diabetes
    Ivana Cvetkovic
    Institute for Biological Research Sinisa Stankovic, 29 Novembra 142, 11000 Belgrade, Serbia and Montenegro
    Endocrinology 146:2942-51. 2005
    ....
  16. pmc The active metabolite of leflunomide, A77 1726, interferes with dendritic cell function
    Bernhard M Kirsch
    Department of Internal Medicine III Clinical Division of Nephrology, Medical University of Vienna, Vienna, Austria
    Arthritis Res Ther 7:R694-703. 2005
    ..These data indicate that interference with several aspects of DC function could significantly contribute to the beneficial effects of leflunomide in inflammatory diseases, including RA...
  17. ncbi 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta
    Christian Peifer
    Department of Pharmacy, Eberhard Karls University, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
    J Med Chem 52:7618-30. 2009
    ..447 microM) possessing differentiated specificity. Selected compounds were profiled over 76 kinases and evaluation of their cellular efficacy showed 18 (CKP138) to be a highly potent and dual-specific inhibitor of CK1delta and p38alpha...
  18. ncbi Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides
    Paul Bamborough
    Epinova DPU, Immuno Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline R and D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK
    J Med Chem 55:587-96. 2012
    ..This proof-of-principle experiment demonstrates the tractability of the BET family and bromodomain target class to fragment-based hit discovery and structure-based lead optimization...
  19. ncbi The pharmacology and safety of paliperidone extended-release in the treatment of schizophrenia
    Edoardo Spina
    Universiy of Messina, Department of Clinical and Experimental Medicine and Pharmacology, Section of Pharmacology, Policlinico Universitario, Via Consolare Valeria, 98125 Messina, Italy
    Expert Opin Drug Saf 6:651-62. 2007
    ..Safety data from elderly patients appear to be promising. Due to negligible hepatic biotransformation, paliperidone ER is unlikely to be involved in clinically significant metabolic drug-drug interactions...
  20. ncbi Risperidone and paliperidone inhibit p-glycoprotein activity in vitro
    Hao Jie Zhu
    Laboratory of Drug Disposition and Pharmacogenetics, Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston, SC, USA
    Neuropsychopharmacology 32:757-64. 2007
    ..In particular, RSP may interact with its own active metabolite PALI by promoting its brain concentration through inhibiting P-gp-mediated efflux of PALI across endothelial cells of the BBB...
  21. ncbi An extrasynaptic GABAA receptor mediates tonic inhibition in thalamic VB neurons
    Fan Jia
    CV Starr Laboratory for Molecular Neuropharmacology, Department of Anesthesiology, Weill Medical College, Cornell University, New York, NY 10021, USA
    J Neurophysiol 94:4491-501. 2005
    ..In view of the critical role of thalamic neurons in the generation of oscillatory activity associated with sleep, these receptors may represent a principal site of action for the novel hypnotic agent gaboxadol...
  22. ncbi Safety and tolerability of oral paliperidone extended-release tablets in elderly patients with schizophrenia: a double-blind, placebo-controlled study with six-month open-label extension
    Andreas Tzimos
    Psychiatric Hospital of Thessaloniki, Thessaloniki, Greece
    Am J Geriatr Psychiatry 16:31-43. 2008
    ..The study was not powered to show statistical differences...
  23. ncbi Modulation of effector cell functions in experimental autoimmune encephalomyelitis by leflunomide--mechanisms independent of pyrimidine depletion
    Thomas Korn
    Department of Neurology, Universitat des Saarlandes, Homburg, Germany
    J Leukoc Biol 76:950-60. 2004
    ..In conclusion, our observations underline that the immunomodulatory potential of leflunomide in effector cells of EAE is clinically relevant and is not exclusively dependent on the depletion of cellular pyrimidine pools...
  24. ncbi Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases
    M L Herrmann
    Rheumatic Autoimmune Disease, Hoechst Marion Roussel Deutschland GmbH, Building H811, D 65926, Frankfurt, Germany
    Immunopharmacology 47:273-89. 2000
    ..This mechanism likely contributes to leflunomide's action as a DMARD in RA and other autoimmune diseases. This review is a summary of current in vivo and in vitro data, focussing primarily on the mechanism of action of leflunomide in RA...
  25. pmc Mechanistic evaluation of the novel HSP90 inhibitor NVP-AUY922 in adult and pediatric glioblastoma
    Nathalie Gaspar
    Signal Transduction and Molecular Pharmacology Team, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 9:1219-33. 2010
    ....
  26. ncbi Paliperidone as a mood stabilizer: a pre-frontal cortex synaptoneurosomal proteomics comparison with lithium and valproic acid after chronic treatment reveals similarities in protein expression
    Maria del Pilar Corena-McLeod
    Neuropsychopharmacology Laboratory, Department of Neuroscience, Mayo Clinic, Jacksonville, FL, USA
    Brain Res 1233:8-19. 2008
    ....
  27. ncbi Practical guidance for dosing and switching paliperidone palmitate treatment in patients with schizophrenia
    S Gopal
    Johnson and Johnson PRD, LLC, 1125 Trenton Harbourton Rd, Titusville, NJ 08560, USA
    Curr Med Res Opin 26:377-87. 2010
    ..This article overviews the recommended dosing strategies for the treatment of schizophrenia patients using the recently FDA-approved once-monthly long-acting injectable atypical antipsychotic, paliperidone palmitate...
  28. ncbi Paliperidone palmitate, a potential long-acting treatment for patients with schizophrenia. Results of a randomized, double-blind, placebo-controlled efficacy and safety study
    Michelle Kramer
    Johnson and Johnson Pharmaceutical Research and Development, L L C, Raritan, NJ, USA
    Int J Neuropsychopharmacol 13:635-47. 2010
    ..PP (50 and 100 mg eq. doses) administered as a gluteal intramuscular injection was efficacious and generally tolerated in these patients with acute symptomatic schizophrenia...
  29. ncbi Population pharmacokinetics of intramuscular paliperidone palmitate in patients with schizophrenia: a novel once-monthly, long-acting formulation of an atypical antipsychotic
    Mahesh N Samtani
    Clinical Pharmacology, Advanced PK PD Modeling and Simulation, Johnson and Johnson Pharmaceutical Research and Development, LLC, 920 Route 202, PRD 2723, Raritan, NJ 08869, USA
    Clin Pharmacokinet 48:585-600. 2009
    ..To characterize the population pharmacokinetics of paliperidone after intramuscular administration of its long-acting palmitate ester at various doses and at two different injection sites (deltoid and gluteal muscle)...
  30. ncbi Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week, placebo-controlled studies
    Herbert Y Meltzer
    Department of Psychiatry, Vanderbilt Medical Center, Nashville, TN, USA
    J Clin Psychiatry 69:817-29. 2008
    ..To evaluate the efficacy and safety of an extended-release (ER) formulation of paliperidone in patients with an acute episode of schizophrenia, in the dosage range of 3 to 15 mg daily...
  31. pmc NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models
    Michael Rugaard Jensen
    Novartis Institutes for BioMedical Research, Oncology Research, Klybeckstrasse 141, CH 4057 Basel, Switzerland
    Breast Cancer Res 10:R33. 2008
    ..HSP90 has emerged in recent years as a promising new target for anticancer therapies...
  32. ncbi Suppression of experimental autoimmune neuritis by leflunomide
    T Korn
    Department of Neurology, Neuroimmunology Branch and MS Clinical Research Group, , Germany
    Brain 124:1791-802. 2001
    ..In summary, leflunomide suppresses EAN efficiently and may constitute a promising therapy for immune-mediated neuropathies...
  33. ncbi A double-blind study of paliperidone palmitate and risperidone long-acting injectable in adults with schizophrenia
    Gahan Pandina
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, New Jersey 08560, USA
    Prog Neuropsychopharmacol Biol Psychiatry 35:218-26. 2011
    ..4 [-1.62;2.38], per-protocol analysis set [primary analysis]). The tolerability and safety of PP was generally similar to RIS-LAI with no new safety or tolerability findings...
  34. ncbi Zonisamide: chemistry, mechanism of action, and pharmacokinetics
    Ilo E Leppik
    MINCEP Epilepsy Care and University of Minnesota, 5775 Wayzata Boulevard, Suite 200, Minneapolis, MN 55416, USA
    Seizure 13:S5-9; discussion S10. 2004
    ..However, since zonisamide is metabolized by cytochrome P450, liver enzyme-inducing AEDs will increase zonisamide clearance, and dosage adjustments may be necessary when it is used in combination with certain AEDs...
  35. ncbi Bile acids induce the expression of the human peroxisome proliferator-activated receptor alpha gene via activation of the farnesoid X receptor
    Ines Pineda Torra
    U 545 Institut National de la Santé et de la Recherche Médicale, Departement d Atherosclerose, Institut Pasteur de Lille, 59019 Lille, France
    Mol Endocrinol 17:259-72. 2003
    ..These results provide molecular evidence for a cross-talk between the FXR and PPARalpha pathways in humans...
  36. ncbi Leflunomide induces apoptosis in fludarabine-resistant and clinically refractory CLL cells
    Sascha Dietrich
    Department of Medicine V, Im Neuenheimer Feld 410, 69120 Heidelberg, Germany
    Clin Cancer Res 18:417-31. 2012
    ..This situation can be mimicked by in vitro stimulation with CD40 ligand (CD40L) and interleukin 4 (IL-4). Our study investigates the impact of the drug leflunomide to overcome apoptosis resistance of CLL cells...
  37. pmc A controlled, evidence-based trial of paliperidone palmitate, a long-acting injectable antipsychotic, in schizophrenia
    Henry A Nasrallah
    Department of Psychiatry, University of Cincinnati College of Medicine, OH 45267, USA
    Neuropsychopharmacology 35:2072-82. 2010
    ..All doses of once-monthly paliperidone palmitate were efficacious and generally tolerated, both locally and systemically. Paliperidone palmitate offers the potential to improve outcomes in adults with symptomatic schizophrenia...
  38. ncbi Zonisamide in the treatment of epilepsy
    Andreas Schulze-Bonhage
    University Hospital Freiburg, Epilepsy Center, Breisacher Str 64, D 79106 Freiburg, Germany
    Expert Opin Pharmacother 11:115-26. 2010
    ..Zonisamide is an antiepileptic drug with multiple mechanisms of action, corresponding to efficacy in diverse epilepsy syndromes...
  39. ncbi Extrasynaptic GABA(A) channels activated by THIP are modulated by diazepam in CA1 pyramidal neurons in the rat brain hippocampal slice
    Catarina E L Lindquist
    Molecular and Cellular Physiology, Department of Physiological Sciences, Lund University, Tornavagen 10 BMC F11, 22184 Lund, Sweden
    Mol Cell Neurosci 24:250-7. 2003
    ..5-5 microM ) of GABA. The increase in the inhibitory conductance with membrane depolarization permits gradation of the shunt pathway relative to the level of the excitatory input...
  40. pmc α7 nicotinic ACh receptors as a ligand-gated source of Ca(2+) ions: the search for a Ca(2+) optimum
    Victor V Uteshev
    Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX 76107, USA
    Adv Exp Med Biol 740:603-38. 2012
    ..In this review, the focus is placed on α7 nAChR-mediated currents and Ca(2+) influx and how this source of Ca(2+) entry compares to NMDA receptors in supporting cytosolic Ca(2+) homeostasis, neuronal function and survival...
  41. ncbi Efficacy and safety of paliperidone palmitate in adult patients with acutely symptomatic schizophrenia: a randomized, double-blind, placebo-controlled, dose-response study
    Srihari Gopal
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, New Jersey 08560, USA
    Int Clin Psychopharmacol 25:247-56. 2010
    ..than placebo (>or=5% difference) were headache, vomiting, extremity pain, and injection site pain. Treatment with paliperidone palmitate (100 mg eq.) was efficacious and all doses tested were tolerable...
  42. pmc Novel HSP90 inhibitors, NVP-AUY922 and NVP-BEP800, radiosensitise tumour cells through cell-cycle impairment, increased DNA damage and repair protraction
    L Stingl
    Klinik für Strahlentherapie der Universität Würzburg, Josef Schneider Strasse 11, D 97080 Wurzburg, Germany
    Br J Cancer 102:1578-91. 2010
    ..The techniques used included cell and colony counts, expression of Hsp90, Hsp70, Akt, survivin, cleaved caspase 3, p53, cell-cycle progression and associated proteins. DNA damage was analysed by histone gammaH2AX and Comet assays...
  43. ncbi Dihydroorotate dehydrogenase inhibitor A771726 (leflunomide) induces apoptosis and diminishes proliferation of multiple myeloma cells
    Philipp Baumann
    Department of Hematology and Oncology, Medizinische Klinik Innenstadt, Klinikum der Universitat Munchen, Munchen, Germany
    Mol Cancer Ther 8:366-75. 2009
    ..Considering the favorable toxicity profile and the great clinical experience with leflunomide in rheumatoid arthritis, this drug represents a potential new candidate for targeted therapy in multiple myeloma...
  44. ncbi Gaboxadol--a new awakening in sleep
    Keith A Wafford
    Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    Curr Opin Pharmacol 6:30-6. 2006
    ..This unique mechanism has contributed to our increased understanding of sleep mechanisms, and targeting of this system offers potential advantages over existing insomnia treatments...
  45. ncbi γ-aminobutyric acid type A receptors that contain the δ subunit promote memory and neurogenesis in the dentate gyrus
    Paul D Whissell
    Institute of Medical Science, University of Toronto, Ontario, Canada
    Ann Neurol 74:611-21. 2013
    ..Accordingly, we sought to determine whether δGABAA receptors regulate memory behaviors, as well as neurogenesis in the DG...
  46. ncbi Farnesoid X receptor inhibits tamoxifen-resistant MCF-7 breast cancer cell growth through downregulation of HER2 expression
    C Giordano
    Centro Sanitario, University of Calabria, Arcavacata di Rende, Italy
    Oncogene 30:4129-40. 2011
    ....
  47. ncbi Differential effects of antipsychotic and antidepressant drugs on neurogenic regions in rats
    Henry A Nasrallah
    Dept of Psychiatry, Univ of Cincinnati College of Medicine, Cincinnati, OH 45267 0521, USA
    Brain Res 1354:23-9. 2010
    ..This olfactory model can be employed in human research as a method to explore the neurogenesis effects of various pharmacologic treatments of neuropsychiatric disorders...
  48. ncbi Paliperidone extended-release tablets in patients with recently diagnosed schizophrenia
    Carla M Canuso
    Ortho McNeil Janssen Scientific Affairs, LLC, Titusville New Jersey, USA
    Early Interv Psychiatry 4:64-78. 2010
    ..Effective early and persistent antipsychotic treatment in recently diagnosed schizophrenia may positively impact long-term outcomes. Paliperidone extended-release (ER) was assessed in this population...
  49. ncbi The role of HLA-DRB1 shared epitope alleles in predicting short-term response to leflunomide in rheumatoid arthritis
    G Saruhan-Direskeneli
    Department of Physiology, Istanbul Faculty of Medicine, Istanbul University, Istanbul, Turkey
    Rheumatology (Oxford) 46:1842-4. 2007
    ..To investigate the role of shared epitope (SE) alleles in the short-term clinical response to leflunomide for the treatment of active RA...
  50. pmc Physiological concentrations of choline activate native alpha7-containing nicotinic acetylcholine receptors in the presence of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea]
    Alexander G Gusev
    Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, IL 62794, USA
    J Pharmacol Exp Ther 332:588-98. 2010
    ..In certain neurological disorders, this activation may be therapeutically beneficial, more efficacious, and safer than treatments with nAChR agonists...
  51. ncbi Use of leflunomide in an allogeneic bone marrow transplant recipient with refractory cytomegalovirus infection
    R K Avery
    Department of Infectious Disease, Cleveland Clinic Foundation, Desk S 32, 9500 Euclid Avenue, Cleveland, OH 44195, USA
    Bone Marrow Transplant 34:1071-5. 2004
    ..However, the toxicity profile of leflunomide in patients with underlying GVHD remains to be defined...
  52. pmc Efficacy of perioperative parecoxib injection on postoperative pain relief after laparoscopic cholecystectomy: a prospective, randomized study
    Thawatchai Akaraviputh
    Department of Surgery, Faculty of Medicine Siriraj Hospital, Mahidol University, Prannok Road, Bangkok, Thailand
    World J Gastroenterol 15:2005-8. 2009
    ..To determine the efficacy of perioperative parecoxib injection on postoperative pain relief after laparoscopic cholecystectomy...
  53. ncbi Treatment of refractory CMV-infection following hematopoietic stem cell transplantation with the combination of foscarnet and leflunomide
    K Ehlert
    University Hospital Muenster, Department of Pediatric Hematology and Oncology, Muenster
    Klin Padiatr 218:180-4. 2006
    ..Here we report the control of refractory CMV disease by the combined use of foscarnet and leflunomide...
  54. ncbi Single doses of parecoxib sodium intravenously are as effective as ketorolac in reducing pain after oral surgery
    Donald R Mehlisch
    SCIREX Corporation, Austin, TX, USA
    J Oral Maxillofac Surg 61:1030-7. 2003
    ....
  55. ncbi Induction of cell growth arrest and apoptotic cell death in human breast cancer MCF-7 cells by the COX-1 inhibitor FR122047
    Hyo Soon Jeong
    Department of Animal Biotechnology, Animal Resources Research Center, and RCTCP, Konkuk University, Gwangjin ku, Seoul 143 701, South Korea
    Oncol Rep 24:351-6. 2010
    ..Our data suggest that the NSAID FR122047 may have an anti-cancer potential in breast cancer...
  56. pmc Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome
    Jose Luis Olmos-Serrano
    Center for Neuroscience Research, Children s National Medical Center, Washington DC, 20010, USA
    J Neurosci 30:9929-38. 2010
    ....
  57. pmc Activation of functional α7-containing nAChRs in hippocampal CA1 pyramidal neurons by physiological levels of choline in the presence of PNU-120596
    Bopanna I Kalappa
    Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, Illinois, United States of America
    PLoS ONE 5:e13964. 2010
    ....
  58. pmc Trypanosoma brucei CTP synthetase: a target for the treatment of African sleeping sickness
    A Hofer
    Medical Biochemistry, Department of Medical Biosciences, Umea University, SE 901 87 Umea, Sweden
    Proc Natl Acad Sci U S A 98:6412-6. 2001
    ..For treatment of sleeping sickness, we propose the use of CTP synthetase inhibitors alone or in combination with appropriate nucleosides or bases...
  59. ncbi Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents
    Ahmed Kamal
    Division of Organic Chemistry, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India
    Eur J Med Chem 46:691-703. 2011
    ..Further some detailed biological assays relating to the cell cycle aspects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of this conjugate...
  60. ncbi Mechanistic study of malononitrileamide FK778 in cardiac transplantation and CMV infection in rats
    Huasong Zeng
    Department of Surgery, University of Chicago, Chicago, IL 60637, USA
    Transplantation 79:17-22. 2005
    ....
  61. ncbi Leflunomide: a drug with a potential beyond rheumatology
    Sven Teschner
    Transplant Center Cologne, University of Cologne, 50924 Cologne, Germany
    Immunotherapy 2:637-50. 2010
    ..This article summarizes the clinical experience with leflunomide in rheumatology and in the evolving field of transplantation...
  62. ncbi A randomized, double-blind, controlled trial on non-opioid analgesics and opioid consumption for postoperative pain relief after laparoscopic cholecystectomy
    S Abdulla
    Department of Anesthesiology and Intensive Care Medicine, Klinikum Bernburg, A Teaching Hospital, Martin Luther University Halle Wittenberg, Kustrenaer Str 98, D 06406 Bernburg, Germany
    Acta Anaesthesiol Belg 63:43-50. 2012
    ....
  63. ncbi Randomized, double-blind, placebo-controlled study of paliperidone extended-release and quetiapine in inpatients with recently exacerbated schizophrenia
    Carla M Canuso
    Ortho McNeil Janssen Scientific Affairs, Titusville, NJ, USA
    Am J Psychiatry 166:691-701. 2009
    ..The authors compared paliperidone extended-release and quetiapine in patients with recently exacerbated schizophrenia requiring hospitalization...
  64. ncbi Isoxazolines and isoxazoles as factor Xa inhibitors
    J R Pruitt
    The DuPont Pharmaceuticals Company, Wilmington, Delaware 19880 0500, USA
    Bioorg Med Chem Lett 10:685-9. 2000
    3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency...
  65. ncbi A randomized, placebo- and active-controlled study of paliperidone extended release for the treatment of acute manic and mixed episodes of bipolar I disorder
    Eduard Vieta
    Institute of Neuroscience, University of Barcelona Hospital Clinic, IDIBAPS, CIBERSAM, Barcelona, Spain
    Bipolar Disord 12:230-43. 2010
    ..To evaluate the antimanic efficacy and safety of paliperidone extended-release (ER) tablets in patients with bipolar I disorder...
  66. ncbi Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes
    Jens Halvard Grønlien
    Oslo Research Park, Oslo, Norway
    Mol Pharmacol 72:715-24. 2007
    ..In summary, our studies reveal two distinct alpha7 PAM profiles, which could offer unique opportunities for modulating alpha7 nAChRs in vivo and in the development of novel therapeutics for central nervous system indications...
  67. pmc Distinct activities of GABA agonists at synaptic- and extrasynaptic-type GABAA receptors
    Martin Mortensen
    Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, UK
    J Physiol 588:1251-68. 2010
    ....
  68. ncbi Reliability, validity and ability to detect change of the clinician-rated Personal and Social Performance scale in patients with acute symptoms of schizophrenia
    Donald L Patrick
    University of Washington, Seattle, WA 98195 9455, USA
    Curr Med Res Opin 25:325-38. 2009
    ..To describe the measurement properties of the Personal and Social Performance scale (PSP), a clinician-reported measure of severity of personal and social dysfunction, in subjects with acute symptoms of schizophrenia...
  69. ncbi Paliperidone for schizophrenia
    Christian Dolder
    School of Pharmacy, Wingate University, Wingate, NC 28174, USA
    Am J Health Syst Pharm 65:403-13. 2008
    ..The efficacy, safety, pharmacology, pharmacokinetics, drug-drug interactions, and administration of paliperidone for schizophrenia are reviewed...
  70. pmc Inhibition of tumour necrosis factor and IL-17 production by leflunomide involves the JAK/STAT pathway
    I Gonzalez-Alvaro
    Rheumatology Unit, Hospital Universitario de la Princesa Madrid, Spain
    Ann Rheum Dis 68:1644-50. 2009
    ..To study the effects of different disease-modifying antirheumatic drugs (DMARD) on different events mediated by IL-15-activated lymphocytes...
  71. ncbi Four-week, double-blind, placebo- and ziprasidone-controlled trial of iloperidone in patients with acute exacerbations of schizophrenia
    Andrew J Cutler
    University of Florida, Gainesville, FL, USA
    J Clin Psychopharmacol 28:S20-8. 2008
    ..Overall, there was improvement in akathisia with iloperidone treatment. Iloperidone treatment was effective, safe, and well tolerated in patients with acute exacerbation of schizophrenia...
  72. ncbi GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic
    Povl Krogsgaard-Larsen
    Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK 2100 Copenhagen, Denmark
    Biochem Pharmacol 68:1573-80. 2004
    ..In this connection, a series of GABA(A) ligands has been developed showing pharmacological profiles ranging from low-efficacy partial GABA(A) agonist activity to selective antagonist effect...
  73. ncbi Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials
    Peter J Weiden
    Center for Cognitive Medicine, Chicago, IL 60612, USA
    J Clin Psychopharmacol 28:S12-9. 2008
    ....
  74. ncbi (89)Zr-trastuzumab PET visualises HER2 downregulation by the HSP90 inhibitor NVP-AUY922 in a human tumour xenograft
    Thijs H Oude Munnink
    Department of Medical Oncology, University of Groningen and University Medical Centre Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands
    Eur J Cancer 46:678-84. 2010
    ..This technique is currently under clinical evaluation and might serve as an early biomarker for HSP90 inhibition in HER2 positive metastatic breast cancer patients...
  75. ncbi Inhibition of polyomavirus BK-specific T-Cell responses by immunosuppressive drugs
    Adrian Egli
    ransplantation and Clinical Virology, Institute for Medical Microbiology, Department of Biomedicine, University of Basel, Basel, Switzerland
    Transplantation 88:1161-8. 2009
    ..Reducing immunosuppression is the treatment of choice for polyomavirus-associated nephropathy in kidney transplant (KT) patients, but strategies and targets are uncertain...
  76. ncbi Properties and inhibition of the first two enzymes of the non-mevalonate pathway of isoprenoid biosynthesis
    C Mueller
    Botanical Institute II, University of Karlsruhe, Kaiserstr 12, D 76128 Karlsruhe, Germany
    Biochem Soc Trans 28:792-3. 2000
    ..The DXR of plants, isolated from barley seedlings, shows a pH optimum of 8.1, which is typical for enzymes active in the chloroplast stroma...
  77. ncbi Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800
    Andrew J Massey
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, Klybeckstrasse 141, WKL 125 2 42, CH 4057 Basel, Switzerland
    Mol Cancer Ther 9:906-19. 2010
    ..Mol Cancer Ther; 9(4); 906-19. (c)2010 AACR...
  78. ncbi The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein
    Jun Sheng Wang
    Laboratory of Drug Disposition and Pharmacogenetics, Department of Psychiatry and Behavioral Sciences, Medical University of South Carolina, Charleston, SC 29425, USA
    Int J Neuropsychopharmacol 7:415-9. 2004
    ..These results indicate that P-gp in the blood-brain barrier significantly influences the brain concentrations of risperidone and 9-OH-risperidone by limiting their CNS access...
  79. pmc Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?
    Christian F Opitz
    Department of Internal Medicine, DRK Kliniken Berlin, Köpenick, Berlin, Germany
    Eur Heart J 29:1936-48. 2008
    ..These characteristics bear more relation to the chemical or pharmacological properties of the drugs than to receptor selectivity itself...
  80. ncbi Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist
    Chengde Wu
    Encysive Pharmaceuticals Inc, 7000 Fannin, Houston, TX 77030, USA
    J Med Chem 47:1969-86. 2004
    ..08 nM), and optimal ET(A)/ET(B) selectivity (441 000-fold). Compound 7z has completed phase-I clinical development and was well tolerated with desirable pharmacokinetics in humans (t(1/2) = 6-7 h, oral availability > 80%)...
  81. ncbi Efficacy and safety of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 52-week open-label studies
    Robin Emsley
    Department of Psychiatry, University of Stellenbosch, Tygerberg, Cape Town, South Africa
    Int Clin Psychopharmacol 23:343-56. 2008
    ..This analysis shows that paliperidone extended-release can maintain improvements in symptoms and functioning and is generally well tolerated for up to 52 weeks in schizophrenia patients...
  82. ncbi NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis
    Suzanne A Eccles
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, United Kingdom
    Cancer Res 68:2850-60. 2008
    ..NVP-AUY922 was glucuronidated less than previously described isoxazoles, yielding higher drug levels in human cancer cells and xenografts. Daily dosing of NVP-AUY922 (50 mg/kg i.p...
  83. ncbi Comparative pharmacology and computational modelling yield insights into allosteric modulation of human alpha7 nicotinic acetylcholine receptors
    David B Sattelle
    MRC Functional Genomics Unit, Department of Physiology, Anatomy and Genetics, University of Oxford, Oxford OX1 3QX, UK
    Biochem Pharmacol 78:836-43. 2009
    ..The new pharmacological findings and computational approaches being developed may inform the design of novel PAM drugs targeting major neurological disorders...
  84. ncbi A randomized, placebo-controlled study to assess the efficacy and safety of 3 doses of paliperidone palmitate in adults with acutely exacerbated schizophrenia
    Gahan J Pandina
    Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ 08560, USA
    J Clin Psychopharmacol 30:235-44. 2010
    ..6% vs 0.0%), and myalgia (1.0% vs 0.0%). The paliperidone palmitate treatment was efficacious and generally tolerated across the dose range (25, 100, or 150 mg eq.) in adult patients with acutely exacerbated schizophrenia...
  85. ncbi Leflunomide inhibits PDK1/Akt pathway and induces apoptosis of human mast cells
    Norifumi Sawamukai
    First Department of Internal Medicine, School of Medicine, University of Occupational and Environmental Health, Kitakyushu, Japan
    J Immunol 179:6479-84. 2007
    ..These results indicate a new way of controlling mast cells and may therefore be the basis for innovative approaches to the treatment of various diseases related to mast cells...
  86. ncbi Leflunomide for polyomavirus type BK nephropathy
    James W Williams
    N Engl J Med 352:1157-8. 2005
  87. ncbi Functional properties of alpha7 nicotinic acetylcholine receptors co-expressed with RIC-3 in a stable recombinant CHO-K1 cell line
    Renza Roncarati
    Discovery Research, Siena Biotech S p A, Siena, Italy
    Assay Drug Dev Technol 6:181-93. 2008
    ..This recombinant cell system is useful for characterization of alpha7 nAChRs and to study the mechanism of action of chemical modulators, in particular the detection of PAMs capable of slowing receptor desensitization kinetics...
  88. ncbi Efficacy and safety of the cyclooxygenase 2 inhibitors parecoxib and valdecoxib in patients undergoing coronary artery bypass surgery
    Elisabeth Ott
    Ischemia Research and Education Foundation, San Francisco, CA 94143, USA
    J Thorac Cardiovasc Surg 125:1481-92. 2003
    ..We prospectively evaluated the safety and efficacy of a newly introduced cyclooxygenase 2 inhibitor in patients undergoing coronary artery bypass grafting surgery through a median sternotomy in a randomized clinical trial...
  89. ncbi Medication satisfaction in schizophrenia: a blinded-initiation study of paliperidone extended release in patients suboptimally responsive to risperidone
    Carla M Canuso
    Ortho McNeil Janssen Scientific Affairs, LLC, 1125 Trenton Harbourton Road A32404, Titusville, NJ 08560, USA
    Int Clin Psychopharmacol 25:155-64. 2010
    ..1%), constipation (7.6%), headache (7.6%) and somnolence (6.6%). Participants with schizophrenia who were suboptimally responsive to risperidone reported improved medication satisfaction after initiation of paliperidone ER...
  90. ncbi Paliperidone extended-release tablets in schizophrenia patients previously treated with risperidone
    Carla M Canuso
    Ortho McNeil Janssen Scientific Affairs LLC, Titusville, NJ, USA
    Int Clin Psychopharmacol 23:209-15. 2008
    ..4% with placebo. In patients who had received risperidone previously but remained sufficiently symptomatic for enrollment, paliperidone ER was significantly more effective than placebo in reducing symptoms and producing functional gains...
  91. ncbi Iloperidone, asenapine, and lurasidone: a brief overview of 3 new second-generation antipsychotics
    Leslie Citrome
    New York University School of Medicine, Department of Psychiatry, New York, NY, USA
    Postgrad Med 123:153-62. 2011
    ..Longer-term and naturalistic studies will be helpful in evaluating these agents and their role in the psychiatric armamentarium...
  92. ncbi Efficacy and tolerability of zonisamide in idiopathic generalized epilepsy
    Ainhoa Marinas
    Fundacion Jimenez Diaz, Madrid, Spain
    Epileptic Disord 11:61-6. 2009
    ..The objective of this study is to evaluate the efficacy and safety of zonisamide (ZNS) for the treatment of idiopathic generalized epilepsies (IGEs)...
  93. ncbi A prospective evaluation of leflunomide therapy for cytomegalovirus disease in renal transplant recipients
    G T John
    Christian Medical College, Department of Nephrology, Vellore, Tamil Nadu, India
    Transplant Proc 37:4303-5. 2005
    ..A prospective evaluation was conducted in renal transplant recipients to study the efficacy of leflunomide in the treatment of CMV disease...
  94. ncbi Preventive effects of perioperative parecoxib on post-discectomy pain
    G Riest
    Klinik für Anästhesiologie und Intensivmedizin, Universitaetsklinikum Essen, Germany
    Br J Anaesth 100:256-62. 2008
    ..Cyclooxygenase inhibitor treatment is viewed increasingly critical because of safety considerations, and there are several open questions on their optimal use...
  95. ncbi The cyclooxygenase isozyme inhibitors parecoxib and paracetamol reduce central hyperalgesia in humans
    Wolfgang Koppert
    Department of Anesthesiology, University Hospital Erlangen, Krankenhausstrasse 12, D 91054 Erlangen, Germany
    Pain 108:148-53. 2004
    ..Thus, besides its well-known effects on inflamed peripheral tissues, inhibition of central COX provides an important mechanism of NSAID-mediated antihyperalgesia in humans...
  96. ncbi Efficacy and tolerability of the new antiepileptic drugs, I: Treatment of new-onset epilepsy: report of the TTA and QSS Subcommittees of the American Academy of Neurology and the American Epilepsy Society
    Jacqueline A French
    Neurological Institute, Hospital of the University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Epilepsia 45:401-9. 2004
    ..S. Food and Drug Administration] in the treatment of children and adults with newly diagnosed partial and generalized epilepsies...
  97. ncbi Lack of analgesic effect of parecoxib following laparoscopic cholecystectomy
    P A E Puolakka
    Department of Anaesthesiology, University Hospital, Tampere, Finland
    Acta Anaesthesiol Scand 50:1027-32. 2006
    ..We studied the effect of a single dose of parecoxib of either 40 or 80 mg in laparoscopic cholecystectomy, and its effect on opioid-induced side-effects...
  98. ncbi The herbicide ketoclomazone inhibits 1-deoxy-D-xylulose 5-phosphate synthase in the 2-C-methyl-D-erythritol 4-phosphate pathway and shows antibacterial activity against Haemophilus influenzae
    Yukiko Matsue
    Biotechnology Research Center, The University of Tokyo, 1 1 1 Yayoi, Bunkyo ku, Tokyo, Japan
    J Antibiot (Tokyo) 63:583-8. 2010
    ..These data reveal the inhibitory mechanism of ketoclomazone on DXP synthase...
  99. pmc ISO-1, a macrophage migration inhibitory factor antagonist, inhibits airway remodeling in a murine model of chronic asthma
    Pei Fen Chen
    Departments of Respiratory Diseases and ShenZhen Third People Hospital, Guangdong, China
    Mol Med 16:400-8. 2010
    ..Our results implicate a possible function of MIF in the pathogenesis of chronic asthma and suggest that MIF might be an important therapeutic target for airway remodeling...
  100. ncbi The effects of paroxetine on the pharmacokinetics of paliperidone extended-release tablets
    J Berwaerts
    Johnson and Johnson Pharmaceutical Research and Development, Titusville, NJ 08560, USA
    Pharmacopsychiatry 42:158-63. 2009
    ..As such, selecting antipsychotic medications with a low potential for drug-drug interactions (DDIs) is crucial, as many are extensively metabolized by hepatic cytochrome P450 (CYP) isozymes...
  101. ncbi A randomized, double-blind, placebo-controlled study of 2 dose ranges of paliperidone extended-release in the treatment of subjects with schizoaffective disorder
    Carla M Canuso
    Johnson and Johnson Pharmaceutical Research and Development, LLC, 1125 Trenton Harbourton Rd E12604, Titusville, NJ 08560, USA
    J Clin Psychiatry 71:587-98. 2010
    ..This study was designed to assess efficacy and safety of paliperidone extended-release (ER) in patients with schizoaffective disorder...

Research Grants65

  1. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  2. DEVELOPING AND IMPROVING INSTITUTIONAL ANIMAL RESOURCES
    PATRICIA SONSALLA; Fiscal Year: 2005
    ..abstract_text> ..
  3. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..benzothiophenes, benzoselenophenes, phthalides, isocoumarins, isochromenes, isoquinolines, quinolines, furans, isoxazoles and various spirotrienones. (3) Aryne annulations will be used to prepare xanthones, thioxanthones and acridones...
  4. Bipolar II Depression: Lithium, SSRI or the Combination
    Susan L McElroy; Fiscal Year: 2010
    ..We also hypothesize that the frequency of side effects will be significantly less in patients on SSRI monotherapy. Thus, secondary aims include assessment of patient satisfaction, which may affect compliance in the clinical setting. ..
  5. Transdisciplinary Imaging Genetics Center (1 of 2)(RMI)
    Steven Potkin; Fiscal Year: 2006
    ..The new knowledge generated by the Center holds considerable promise for improving diagnosis and treatment of mental illness. [unreadable] [unreadable]..
  6. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  7. Rehabilitation of Spinal Cord Injury-Related Pain
    Mark Jensen; Fiscal Year: 2006
    ..abstract_text> ..
  8. Human 5HT 1E Serotonin Receptor Drug Development (RMI)
    Milt Teitler; Fiscal Year: 2005
    ..Selective agonists and antagonists for the 5HT1E receptor should, at the least, provide information on the function of this highly expressed receptor, and may lead to novel therapeutics for brain dysfunction. ..
  9. The role of dendritic cell-T cell interactions in the p*
    Mariana Kaplan; Fiscal Year: 2006
    ..These could lead into the development of novel therapeutic interventions designed to reverse these abnormalities and abrogate or block the onset and/or severity of this disease. ..
  10. CMV DISRUPTION OF CONSTITUTIVE MHC CLASS II
    W Waldman; Fiscal Year: 2004
    ....
  11. Zonisamide for Weight Reduction in Obese Adults
    Kishore Gadde; Fiscal Year: 2009
    ..We will also systematically assess whether weight loss achieved with zonisamide treatment can reduce metabolic and cardiovascular risk factors. ..
  12. TNF-alpha modulator as a radioprotector in liver
    Jiajiu Shaw; Fiscal Year: 2006
    ..The ultimate goal is to develop a radioprotective drug to be used in conjunction with radio therapy. [unreadable] [unreadable] [unreadable]..
  13. Feasibility Study of Three NCEs for Rheumatoid Arthritis
    Jiajiu Shaw; Fiscal Year: 2004
    ..Ultimately, the successful drug candidate will provide a significantly improved therapy for patients suffering from Rheumatoid Arthritis. ..
  14. Development of UTL-5b for Rheumatoid Arthritis: Mechanism of Action
    Jiajiu Shaw; Fiscal Year: 2007
    ..This phase 1 study will focus on a comprehensive collagen-induced arthritis animal study. [unreadable] [unreadable] [unreadable]..
  15. Evaluation of models of pharmacoresistant epilepsy.
    H White; Fiscal Year: 2005
    ..abstract_text> ..
  16. Stigma & Quality of Life of Youth w/Facial Differences
    Donald Patrick; Fiscal Year: 2005
    ..Participants for this study will be recruited from sites in Seattle, Chicago, and Chapel Hill, NC. ..
  17. Management of Chronic Pain in Rehabilitation Medicine
    Mark Jensen; Fiscal Year: 2006
    ..A Scientific Core will provide scientific direction, project coordination, data collection and management, statistical support, and shared scientific expertise. ..
  18. Mechanisms of T-cell induced-APC cytotoxicity in lupus
    Mariana Kaplan; Fiscal Year: 2006
    ..The sponsor and the institution are committed to contributing protected time, career development and resources to the applicant. ..
  19. Long-term antidepressant outcome in bipolar depression
    NASSIR GHAEMI; Fiscal Year: 2005
    ..In this process, the applicant will develop competence to lead independent studies of the long-term treatment of bipolar disorder as a principal investigator. ..
  20. Molecular Biology of 5HT2A receptor expressing synapses
    Milt Teitler; Fiscal Year: 2005
    ....
  21. Nanoparticle targeting of cathepsin-L inhibitor and doxorubicin in breast cancer
    Shaker Mousa; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  22. PROSPECTIVE STUDY OF TARDIVE DYSKINESIA DEVELOPMENT
    John Kane; Fiscal Year: 2001
    ..This strategy will provide a rapid and cost-effective answer to a critical question. ..
  23. ANTIVIRAL ACTIVITY OF THE IMMUNOSUPPRESSANT LEFLUNOMIDE
    W Waldman; Fiscal Year: 2004
    ....
  24. Hearing Loss and Quality of Life of Children and Youth
    Donald Patrick; Fiscal Year: 2009
    ....
  25. Quality of Life of Overweight Youth: Multicultural View
    Donald Patrick; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  26. Quality Life Among Youth with Craniofacial Conditions
    Donald Patrick; Fiscal Year: 2004
    ..S., and one in the United Kingdom. Adolescents and their parents will complete questionnaires at baseline, and gain at 1-2 year clinical follow-up. ..
  27. Serotonin-related genes in human brain
    Wolfgang Sadee; Fiscal Year: 2008
    ..Identifying genetic variants that regulate key serotonin-related genes will be a significant step toward developing new methods for the diagnosis, treatment and, possibly, prevention of these disorders. [unreadable] [unreadable]..
  28. Altered Function of a GABA-A receptor epilepsy mutation
    Mathew Jones; Fiscal Year: 2007
    ..abstract_text> ..
  29. Role of ephrins in lung edema due to virus and hypoxia
    Todd Carpenter; Fiscal Year: 2008
    ..These studies will explore novel mechanisms contributing to pulmonary edema formation and may ultimately identify potential sites of therapeutic intervention in that process. [unreadable] [unreadable]..
  30. Micellar VIP Nanoparticles for Rheumatoid Arthritis
    Israel Rubinstein; Fiscal Year: 2007
    ..abstract_text> ..
  31. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  32. 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. ..
  33. Alcohol-specific modifications of glycated Hb: Novel biomarkers of alcohol abuse
    Yousef Al Abed; Fiscal Year: 2007
    ..Future studies will be designed to measure these alcohol-specific-markers in humans following binge and chronic alcohol intake. [unreadable] [unreadable] [unreadable]..
  34. Cross-Coupling Reactions of Organosilanols
    SCOTT DENMARK; Fiscal Year: 2009
    ..Synthetic approaches to isodomoic acid H, hepatitis C viral inihibiting indole alkaloids, the salicylihalimide macrolactone oximidine II, and polyene antiviral antibiotic viridenomycin are detailed. ..
  35. Eliciting Patient Treatment Preferences for Osteoporosis
    Liana Fraenkel; Fiscal Year: 2008
    ..abstract_text> ..
  36. Dysfunctional Cortico-Limbic Activity and Connectivity in Bipolar Disorder and Li
    Amit Anand; Fiscal Year: 2010
    ..This study will also establish an experimental paradigm to study brain connectivity which could be used to investigate other disorders. ..
  37. Prevalence and Treatment of Hypovitaminosis D in RA
    Karen Hansen; Fiscal Year: 2008
    ..abstract_text> ..
  38. Anesthetic Effects on Thalamic Synaptic Transmission
    PETER GOLDSTEIN; Fiscal Year: 2008
    ..By better understanding how anesthetic agents interact with specific subunits of the GABA-A receptor in different regions of the brain, it may be possible to design more selective, and therefore safer, anesthetics. ..
  39. Hybrid Drugs: Novel Pharmacotherapy for ADHD
    FRANK TARAZI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  40. Polymorphisms in Regulatory Regions of Addiction Genes
    Wolfgang Sadee; Fiscal Year: 2005
    ..The results will permit us to assign functional significance to cis-regulatory polymorphisms as a guide in clinical association studies of drug addiction. ..
  41. Tandem Cycloaddition Chemistry of 2-Azoniaheterodienes
    SCOTT DENMARK; Fiscal Year: 2007
    ..abstract_text> ..
  42. MECHANISMS OF SULFATE TRANSPORT AND REGULATION
    Michael Jennings; Fiscal Year: 2007
    ..abstract_text> ..
  43. Molecular Mechanisms Underlying Age-Related Hearing Loss
    Jianxin Bao; Fiscal Year: 2004
    ..The ultimate goal of this research is to develop methods for prevention and treatment of age-related loss of SGNs, based on identifying molecular candidates involved in this aging process. ..
  44. EFFECT OF VIRUS AND HYPOXIA ON LUNG ENDOTHELIN AND EDEMA
    Todd Carpenter; Fiscal Year: 2004
    ..abstract_text> ..
  45. Pulmonary Hypertension Scientific Conference
    Michael McGoon; Fiscal Year: 2004
    ....
  46. MUTATIONS OF MUSCARINIC CHOLINERGIC RECEPTOR GENES
    Wolfgang Sadee; Fiscal Year: 2001
    ..The expected insights from the studies outlined in this proposal should assist in the design of cholinergic therapy for cognitive disorders. ..
  47. Novel pharmacotherapies for treatment of ADHD
    FRANK TARAZI; Fiscal Year: 2003
    ..Expected findings should evolve new principles and lead to novel compounds that can be used as much-needed innovative treatments for ADHD and other major neuropsychiatric disorders. ..
  48. GENETIC DETERMINATION OF ALLOGRAFT VASCULOPATHY
    Raymond Benza; Fiscal Year: 2002
    ..If his faculty mentor were to leave the institution, a new mentor will be appointed and his continued development toward becoming a independent physician scientist supported and encouraged. ..
  49. DIABETIC AUTONOMIC NEUROPATHY
    Phillip Low; Fiscal Year: 2001
    ..abstract_text> ..
  50. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  51. Effects of antipsychotic drugs on brain and behavior
    FRANK TARAZI; Fiscal Year: 2005
    ..adult rats, and should evolve new principles for improved treatments for childhood-onset schizophrenia and other major pediatric psychiatric disorders. ..
  52. The Role of TIMP-1 in Uterine Physiology
    Warren Nothnick; Fiscal Year: 2005
    ..These studies will broaden our understanding on the role of TIMP-1 in uterine physiology and may help to develop new strategies to treat uterine disorders such as infertility, endometriosis and uterine cancer. ..
  53. Antipsychotic Actions in Models of NMDA Hypofunction
    Gary Duncan; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  54. Roles of Neuregulin in Age Related Hearing Loss
    Jianxin Bao; Fiscal Year: 2005
    ..The goal of this award is to elucidate the role of NRG-CD in age-related loss of SGNs as well as to provide the candidate with the continuity of support necessary to develop into an independent investigator. ..
  55. RUPP-PI Project
    Michael Aman; Fiscal Year: 2006
    ..S.U. also plans two pilot studies: (a) a randomized clinical trial in 60 children with PDDs and severe ADHD behavior and (b) a study of ziprasidone in 30 children and adolescents with PDDs and highly irritable behaviors. ..
  56. Substance Abuse in ADHD Girls
    Timothy Wilens; Fiscal Year: 2006
    ..Thus, the research, approach, and goals of this R01 application are consistent with those underscored in the PA and by the Institute of Medicine as being of the highest research priority. ..
  57. Ligands to study the glutamate receptor and transporters
    NICHOLAS NATALE; Fiscal Year: 2006
    ..And also relevant to the special considerations for the AREA program, our research group has had a significant positive impact on the participation of University of Idaho students in research. [unreadable] [unreadable]..
  58. OPIOID RECEPTOR REGULATION
    Wolfgang Sadee; Fiscal Year: 2003
    ..Considered together, these hypotheses may yield important insights into the mechanisms underlying tolerance and dependence, providing the opportunity to develop effective therapies of narcotic addiction. ..
  59. PROGNOSIS OF CHILDREN WITH A FIRST UNPROVOKED SEIZURE
    Shlomo Shinnar; Fiscal Year: 2002
    ....
  60. Estrogen regulation of uterine microRNAs: Novel factors in MMP-9 regulation
    Warren Nothnick; Fiscal Year: 2008
    ..Enhancing our understanding on the regulation of MMP-9 expression may lead to the establishment of novel approaches to counteract mis-expression of this protease and the diseases associated with it. [unreadable] [unreadable] [unreadable]..
  61. Studying nicotinic AChRs in histaminergic neurons
    VICTOR UTESHEV GAARD; Fiscal Year: 2007
    ..Some of these effects of nicotine and therapeutic nicotinic agents may arise from their ability to modulate histaminergic function. [unreadable] [unreadable]..
  62. The impact of the pneumococcal conjugate vaccine on pneumonia hospitalizations
    CARLOS GRIJALVA; Fiscal Year: 2008
    ..We propose the use of NIS and SID for the evaluation of the pneumococcal conjugate vaccination program, using an innovative approach. [unreadable] [unreadable] [unreadable] [unreadable]..
  63. DOPAMINERGIC NEUROTOXINS AND AGING
    PATRICIA SONSALLA; Fiscal Year: 2004
    ..These studies will provide novel and relevant Information as to the contribution of VMAT2-containing vesicles in neuroprotection as well as in neurodegeneration under conditions of a metabolic stress. ..
  64. Adenosine, Glutamate and Neurodegeneration
    PATRICIA SONSALLA; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  65. Dopamine Homeostasis, Vesicles & Neurodegeneration
    PATRICIA SONSALLA; Fiscal Year: 2004
    ..Results from these studies will provide novel and relevant information as to the contribution of VMAT2 containing vesicles in neuroprotection as well as in neurodegeneration of DA neurons during metabolic stress. ..