piperidines

Summary

Summary: A family of hexahydropyridines.

Top Publications

  1. pmc Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer
    Samuel A Wells
    Dept of Surgery, Washington University School of Medicine, Box 8109, 660 S Euclid Ave, St Louis, MO 63110, USA
    J Clin Oncol 28:767-72. 2010
  2. ncbi Phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) or adalimumab monotherapy versus placebo in patients with active rheumatoid arthritis with an inadequate response to disease-modifying antirheumatic drugs
    Roy Fleischmann
    Metroplex Clinical Research Center and University of Texas Southwestern Medical Center, Dallas, TX 75231, USA
    Arthritis Rheum 64:617-29. 2012
  3. pmc Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects
    Jonathan Z Long
    The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nat Chem Biol 5:37-44. 2009
  4. ncbi Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study
    K A Papp
    Probity Medical Research, 135 Union Street East, Waterloo, ON N2J 1C4, Canada
    Br J Dermatol 167:668-77. 2012
  5. ncbi A phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) versus placebo in combination with background methotrexate in patients with active rheumatoid arthritis and an inadequate response to methotrexate alone
    Joel M Kremer
    Albany Medical College, Albany, New York 12206, USA
    Arthritis Rheum 64:970-81. 2012
  6. ncbi FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis
    Max Hasmann
    Fujisawa GmbH, Neumarkter Strasse 61, 81673 Munich, Germany
    Cancer Res 63:7436-42. 2003
  7. ncbi The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo
    Joel M Kremer
    Albany Medical College, Albany, New York, USA
    Arthritis Rheum 60:1895-905. 2009
  8. pmc Transcription inhibition by flavopiridol: mechanism of chronic lymphocytic leukemia cell death
    Rong Chen
    Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Blood 106:2513-9. 2005
  9. ncbi Endogenous cannabinoids mediate retrograde signalling at hippocampal synapses
    R I Wilson
    Nature 410:588-92. 2001
  10. pmc Combined vascular endothelial growth factor receptor and epidermal growth factor receptor (EGFR) blockade inhibits tumor growth in xenograft models of EGFR inhibitor resistance
    George N Naumov
    Children s Hospital, Division of Hematology Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School, and Massachusetts General Hospital Cancer Center, Boston, MA, USA
    Clin Cancer Res 15:3484-94. 2009

Research Grants

Detail Information

Publications390 found, 100 shown here

  1. pmc Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer
    Samuel A Wells
    Dept of Surgery, Washington University School of Medicine, Box 8109, 660 S Euclid Ave, St Louis, MO 63110, USA
    J Clin Oncol 28:767-72. 2010
    ..These results demonstrate that vandetanib may provide an effective therapeutic option in patients with advanced hereditary MTC, a rare disease for which there has been no effective therapy...
  2. ncbi Phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) or adalimumab monotherapy versus placebo in patients with active rheumatoid arthritis with an inadequate response to disease-modifying antirheumatic drugs
    Roy Fleischmann
    Metroplex Clinical Research Center and University of Texas Southwestern Medical Center, Dallas, TX 75231, USA
    Arthritis Rheum 64:617-29. 2012
    ....
  3. pmc Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects
    Jonathan Z Long
    The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Nat Chem Biol 5:37-44. 2009
    ..These data indicate that 2-AG endogenously modulates several behavioral processes classically associated with the pharmacology of cannabinoids and point to overlapping and unique functions for 2-AG and anandamide in vivo...
  4. ncbi Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study
    K A Papp
    Probity Medical Research, 135 Union Street East, Waterloo, ON N2J 1C4, Canada
    Br J Dermatol 167:668-77. 2012
    ..Tofacitinib is a novel, oral Janus kinase inhibitor under investigation as a potential treatment for plaque psoriasis...
  5. ncbi A phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) versus placebo in combination with background methotrexate in patients with active rheumatoid arthritis and an inadequate response to methotrexate alone
    Joel M Kremer
    Albany Medical College, Albany, New York 12206, USA
    Arthritis Rheum 64:970-81. 2012
    ....
  6. ncbi FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis
    Max Hasmann
    Fujisawa GmbH, Neumarkter Strasse 61, 81673 Munich, Germany
    Cancer Res 63:7436-42. 2003
    ....
  7. ncbi The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo
    Joel M Kremer
    Albany Medical College, Albany, New York, USA
    Arthritis Rheum 60:1895-905. 2009
    ....
  8. pmc Transcription inhibition by flavopiridol: mechanism of chronic lymphocytic leukemia cell death
    Rong Chen
    Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Blood 106:2513-9. 2005
    ..The dependence of CLL-cell survival on short-lived oncoproteins may provide the biochemical basis for the therapeutic index in response to flavopiridol...
  9. ncbi Endogenous cannabinoids mediate retrograde signalling at hippocampal synapses
    R I Wilson
    Nature 410:588-92. 2001
    ..Signalling by the endocannabinoid system thus represents a mechanism by which neurons can communicate backwards across synapses to modulate their inputs...
  10. pmc Combined vascular endothelial growth factor receptor and epidermal growth factor receptor (EGFR) blockade inhibits tumor growth in xenograft models of EGFR inhibitor resistance
    George N Naumov
    Children s Hospital, Division of Hematology Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School, and Massachusetts General Hospital Cancer Center, Boston, MA, USA
    Clin Cancer Res 15:3484-94. 2009
    ..EGFR TKI resistance is not completely understood and has been associated with certain EGFR and K-RAS mutations and MET amplification...
  11. ncbi Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis
    William J Sandborn
    Division of Gastroenterology, University of California San Diego, 9500 Gilman Dr, La Jolla, CA 92093 0956, USA
    N Engl J Med 367:616-24. 2012
    ..These cytokines are integral to lymphocyte activation, function, and proliferation...
  12. ncbi A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feeding
    Raquel Gomez
    University Institute of Drug Dependencies, Department of Psychobiology, University Complutense of Madrid, Madrid 28223, Spain
    J Neurosci 22:9612-7. 2002
    ..Pretreatment with SR141716A enhanced the inhibition of feeding induced by intraperitoneal administration of oleoylethanolamide. The results reveal an unexpected role for peripheral CB1 receptors in the regulation of feeding...
  13. ncbi ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration
    Stephen R Wedge
    Department of Cancer and Infection Research, AstraZeneca, Cheshire SK10 4TG, United Kingdom
    Cancer Res 62:4645-55. 2002
    ..4 cm(3) volume. ZD6474 is currently in Phase I clinical development as a once-daily oral therapy in patients with advanced cancer...
  14. pmc The cannabinoid CB1 receptor antagonist SR141716 blocks the orexigenic effects of intrahypothalamic ghrelin
    Sonia A Tucci
    School of Psychology, University of Liverpool, Eleanor Rathbone Building, Bedford Street South, Liverpool L69 7ZA
    Br J Pharmacol 143:520-3. 2004
    ....
  15. ncbi Flavopiridol inhibits P-TEFb and blocks HIV-1 replication
    S H Chao
    Molecular Biology Program and the Department of Biochemistry, University of Iowa, Iowa City, Iowa 52242, USA
    J Biol Chem 275:28345-8. 2000
    ..Furthermore, flavopiridol blocked HIV-1 replication in both single-round and viral spread assays with an IC(50) of less than 10 nm...
  16. ncbi Vandetanib plus pemetrexed for the second-line treatment of advanced non-small-cell lung cancer: a randomized, double-blind phase III trial
    Richard H de Boer
    Western Hospital, Melbourne, Australia
    J Clin Oncol 29:1067-74. 2011
    ..This randomized, placebo-controlled phase III study assessed the efficacy of vandetanib plus pemetrexed as second-line therapy in advanced non-small-cell lung cancer...
  17. ncbi Retrograde inhibition of presynaptic calcium influx by endogenous cannabinoids at excitatory synapses onto Purkinje cells
    A C Kreitzer
    Department of Neurobiology, Harvard Medical School, Boston, MA 02115, USA
    Neuron 29:717-27. 2001
    ..DSE may provide a way for cells to use their firing rate to dynamically regulate synaptic inputs. Together with previous studies, these findings suggest a widespread role for endogenous cannabinoids in retrograde synaptic inhibition...
  18. ncbi Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia
    Jean Pierre Despres
    Quebec Heart Institute, Laval Hospital Research Center, and the Division of Kinesiology, Department of Social and Preventive Medicine, Laval University, Ste Foy, Que, Canada
    N Engl J Med 353:2121-34. 2005
    ..The Rimonabant in Obesity-Lipids (RIO-Lipids) study examined the effects of rimonabant on metabolic risk factors, including adiponectin levels, in high-risk patients who are overweight or obese and have dyslipidemia...
  19. ncbi Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials
    Robin Christensen
    The Parker Institute, Musculoskeletal Statistics Unit, Frederiksberg Hospital, Frederiksberg, Denmark
    Lancet 370:1706-13. 2007
    ..We did a meta-analysis of all published randomised controlled trials to assess the efficacy and safety of the newly approved anti-obesity agent rimonabant...
  20. pmc Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential
    Laetitia Mony
    Laboratoire de Neurobiologie, Ecole Normale Superieure, CNRS, Paris, France
    Br J Pharmacol 157:1301-17. 2009
    ..A better understanding of how NR2B-containing NMDARs (and NMDARs in general) operate and how they can be modulated should help define new strategies to counteract the deleterious effects of dysregulated NMDAR activity...
  21. ncbi Lack of significant effect of bilastine administered at therapeutic and supratherapeutic doses and concomitantly with ketoconazole on ventricular repolarization: results of a thorough QT study (TQTS) with QT-concentration analysis
    Benoit Tyl
    Robert Ballanger s Hospital, Department of Cardiology, Aulnay sous Bois, France
    J Clin Pharmacol 52:893-903. 2012
    ..3 ms; UCL, 12.16 ms). This result was most likely related to the cardiac effect of ketoconazole because for all time points, bilastine plasma concentrations were lower than those observed following the supratherapeutic dose...
  22. ncbi The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies
    Aimable Nahimana
    Service of Hematology, University Hospital of Lausanne, Lausanne, Switzerland
    Blood 113:3276-86. 2009
    ..The results support the potential of APO866 for treating hematologic malignancies...
  23. ncbi Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study
    T Zuberbier
    Department of Dermatology and Allergy, Charite Universitatsmedizin Berlin, Germany
    Allergy 65:516-28. 2010
    ..The aim of this study was to compare the clinical efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg and placebo in CU patients with moderate-to-severe symptoms...
  24. pmc Effectiveness and tolerability of high-dose (23 mg/d) versus standard-dose (10 mg/d) donepezil in moderate to severe Alzheimer's disease: A 24-week, randomized, double-blind study
    Martin R Farlow
    Department of Neurology, Indiana University School of Medicine, Indianapolis, 46202, USA
    Clin Ther 32:1234-51. 2010
    ..We hypothesized that the loss of initial therapeutic benefit over time may be mitigated by higher doses of a cholinesterase inhibitor...
  25. pmc Endocannabinoids in the rat basolateral amygdala enhance memory consolidation and enable glucocorticoid modulation of memory
    Patrizia Campolongo
    Department of Physiology and Pharmacology, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy
    Proc Natl Acad Sci U S A 106:4888-93. 2009
    ..c.). These findings indicate that endocannabinoids in the BLA enhance memory consolidation and suggest that CB1 activity within this brain region is required for enabling glucocorticoid effects on memory consolidation enhancement...
  26. ncbi Modulation of anxiety through blockade of anandamide hydrolysis
    Satish Kathuria
    Department of Pharmacology, University of California, Irvine, California, USA
    Nat Med 9:76-81. 2003
    ..Our results indicate that anandamide participates in the modulation of emotional states and point to fatty acid amide hydrolase inhibition as an innovative approach to anti-anxiety therapy...
  27. ncbi Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients
    C Bachert
    Department of Oto Rhino Laryngology, Ghent University Hospital, Ghent, Belgium
    Allergy 64:158-65. 2009
    ..The objective of this study was to compare the efficacy and safety of bilastine 20 mg vs placebo and desloratadine 5 mg in subjects with seasonal allergic rhinitis (SAR)...
  28. ncbi Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study
    P Kuna
    Division of Internal Medicine, Asthma and Allergy, Barlicki University Hospital, Lodz, Poland
    Clin Exp Allergy 39:1338-47. 2009
    ..Bilastine is a new non-sedative H(1) receptor antagonist, indicated for the treatment of allergic rhinitis (AR) (seasonal and perennial)...
  29. ncbi Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor
    Paul S Changelian
    Immunology Group, Department of Antibacterials and Immunology, Pfizer Global Researchand Development, Groton, CT 06340, USA
    Science 302:875-8. 2003
    ..On the basis of these preclinical results, we believe JAK3 blockade by CP-690,550 has potential for therapeutically desirable immunosuppression in human organ transplantation and in other clinical settings...
  30. ncbi Endocannabinoid control of food intake and energy balance
    Vincenzo Di Marzo
    Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, 80078, Pozzuoli, Naples, Italy
    Nat Neurosci 8:585-9. 2005
    ..Here we discuss the multifaceted regulation of energy homeostasis by endocannabinoids, together with its applications to the treatment of eating disorders and metabolic syndromes...
  31. ncbi A 1-year, randomized, placebo-controlled study of donepezil in patients with mild to moderate AD
    B Winblad
    Karolinska Institutet, Alzheimer s Disease Research Center, Division of Geriatric Medicine, Huddinge Hospital B, Stockholm, Sweden
    Neurology 57:489-95. 2001
    ..To evaluate the long-term clinical efficacy and safety of donepezil versus placebo over 1 year in patients with mild to moderate AD...
  32. pmc Vandetanib plus docetaxel versus docetaxel as second-line treatment for patients with advanced non-small-cell lung cancer (ZODIAC): a double-blind, randomised, phase 3 trial
    Roy S Herbst
    Department of Thoracic Head and Neck Medical Oncology, University of Texas MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 432, Houston, TX 77030 4009, USA
    Lancet Oncol 11:619-26. 2010
    ..These results supported investigation of the combination in this larger, definitive phase 3 trial (ZODIAC)...
  33. pmc Phase II study of flavopiridol in relapsed chronic lymphocytic leukemia demonstrating high response rates in genetically high-risk disease
    Thomas S Lin
    Division of Hematology and Oncology, The Ohio State University, Columbus, OH 43210, USA
    J Clin Oncol 27:6012-8. 2009
    ..Given the relevance of these findings to treating genetically high-risk CLL, a prospective confirmatory study was initiated...
  34. pmc Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase
    Tracy L Keller
    Department of Developmental Biology, Harvard School of Dental Medicine, Boston, Massachusetts, USA
    Nat Chem Biol 8:311-7. 2012
    ..This work both explains the molecular mechanism of a promising family of therapeutics and highlights the AAR pathway as an important drug target for promoting inflammatory resolution...
  35. ncbi Alogliptin added to insulin therapy in patients with type 2 diabetes reduces HbA(1C) without causing weight gain or increased hypoglycaemia
    J Rosenstock
    Dallas Diabetes and Endocrine Center, Dallas, TX 75230, USA
    Diabetes Obes Metab 11:1145-52. 2009
    ..To assess the efficacy and safety of alogliptin added to insulin in patients with type 2 diabetes inadequately controlled with insulin alone or combined with metformin...
  36. ncbi Donepezil, an acetylcholinesterase inhibitor against Alzheimer's dementia, promotes angiogenesis in an ischemic hindlimb model
    Yoshihiko Kakinuma
    Department of Cardiovascular Control, Kochi Medical School, Nankoku, Kochi 783 8505, Japan
    J Mol Cell Cardiol 48:680-93. 2010
    ..The present study concludes that donepezil can act as a therapeutic tool to accelerate angiogenesis in cardiovascular disease patients...
  37. pmc Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response
    Mark S Sundrud
    Department of Pathology, Harvard Medical School and Immune Disease Institute, Boston, MA 02115, USA
    Science 324:1334-8. 2009
    ..These results indicate that the AAR pathway is a potent and selective regulator of inflammatory T cell differentiation in vivo...
  38. ncbi Effect of alogliptin, pioglitazone and glargine on pancreatic β-cells in diabetic db/db mice
    Satoshi Kawashima
    Department of Metabolic Medicine, Osaka University Graduate School of Medicine, 2 2 Yamadaoka, Suita City, Osaka 565 0871, Japan
    Biochem Biophys Res Commun 404:534-40. 2011
    ..To examine if anti-diabetic reagents, such as insulin, pioglitazone (pio), and alogliptin (alo), have protective effects on β-cell mass and function in vivo, we treated obese diabetic db/db mice with these reagents...
  39. ncbi Randomized phase II study of vandetanib alone or with paclitaxel and carboplatin as first-line treatment for advanced non-small-cell lung cancer
    John V Heymach
    Dana Farber Cancer Institute, Boston, MA 02115, USA
    J Clin Oncol 26:5407-15. 2008
    ..The antitumor activity of vandetanib monotherapy or vandetanib with paclitaxel and carboplatin (VPC) was compared with paclitaxel and carboplatin (PC) in previously untreated patients with non-small-cell lung cancer (NSCLC)...
  40. ncbi Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers
    Silke Conen
    Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands
    J Psychopharmacol 25:1517-23. 2011
    ..Bilastine did not produce any driving impairment after single and repeated doses and can be safely used in traffic in doses up to 40 mg...
  41. ncbi Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine
    Nerea Jauregizar
    PharmaDatum Data Análisis SL, Bermeo, Spain
    Clin Pharmacokinet 48:543-54. 2009
    ..To model the pharmacokinetic and pharmacodynamic relationship of bilastine, a new histamine H(1) receptor antagonist, from single- and multiple-dose studies in healthy adult subjects...
  42. ncbi Peripheral endocannabinoid system-mediated actions of rimonabant on growth hormone secretion are ghrelin-dependent
    O Al-Massadi
    Instituto de Investigaciones Sanitarias, Complejo Hospitalario Universitario de Santiago de Compostela, SERGAS, Santiago de Compostela, Spain
    J Neuroendocrinol 22:1127-36. 2010
    ..In conclusion, the data reported in the present study establish, from a physiological point of view, the existence of a novel mechanism of GH regulation implicating the action of the cannabinoid receptor on the somatotroph axis...
  43. pmc Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain
    S G Kinsey
    Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia, USA
    J Pharmacol Exp Ther 330:902-10. 2009
    ..These data indicate that inhibition of FAAH and MAGL reduces neuropathic pain through distinct receptor mechanisms of action and present viable targets for the development of analgesic therapeutics...
  44. ncbi Short-term infusion of the mu-opioid agonist remifentanil in humans causes hyperalgesia during withdrawal
    Martin S Angst
    Department of Anesthesia, Stanford University School of Medicine, 300 Pasteur Drive, Stanford, CA 94305, USA
    Pain 106:49-57. 2003
    ..This study also points to a differential susceptibility of different pain modalities for the expression of hyperalgesia associated with opioid administration...
  45. ncbi Depression-like phenotype following chronic CB1 receptor antagonism
    Chad E Beyer
    Pfizer Global Research and Development, Princeton, NJ 08543, USA
    Neurobiol Dis 39:148-55. 2010
    ..These preclinical findings mimic clinical reports and implicate possible mechanisms responsible for the unfavorable psychiatric events reported following chronic rimonabant use...
  46. pmc Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia
    John C Byrd
    Division of Hematology Oncology, Department of Internal Medicine, The Ohio State University, Columbus, OH 43210, USA
    Blood 109:399-404. 2007
    ..Patients with bulky disease and high-risk genetic features have achieved durable responses, thereby justifying further study of flavopiridol in CLL and other diseases...
  47. ncbi Differential role of anandamide and 2-arachidonoylglycerol in memory and anxiety-like responses
    Arnau Busquets-Garcia
    Facultat de Ciencies de la Salut i de la Vida, Universitat Pompeu Fabra, Barcelona, Spain
    Biol Psychiatry 70:479-86. 2011
    ..An alternative approach to circumvent this limitation consists of enhancing the concentration of the endocannabinoids anandamide and 2-arachidonoylglycerol...
  48. ncbi Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells
    Basant Kumar Thakur
    Department of Pediatrics, Hematology and Oncology, Hannover Medical School, Carl Neuberg Str 1, 30625 Hannover, Germany
    Biochem Biophys Res Commun 424:371-7. 2012
    ....
  49. ncbi Cannabinoid receptor 1 (CB1) antagonism enhances glucose utilisation and activates brown adipose tissue in diet-induced obese mice
    M Bajzer
    Metabolic Diseases Institute, University of Cincinnati, 2140 East Galbraith Road, Building B, Room 332, Cincinnati, OH 45237 1625, USA
    Diabetologia 54:3121-31. 2011
    ....
  50. ncbi Efficacy and safety of alogliptin added to metformin in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label, long-term extension study
    Y Seino
    Kansai Electric Power Hospital, Osaka, Japan
    Diabetes Obes Metab 14:927-36. 2012
    ..To evaluate the efficacy and safety of alogliptin added to metformin versus metformin monotherapy in Japanese patients with type 2 diabetes who achieved inadequate glycaemic control on metformin (500 or 750 mg/day) + diet/exercise...
  51. ncbi Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis
    Joaquin Sastre
    Allergy Department, Fundacion Jimenez Diaz, Madrid, Spain
    Curr Med Res Opin 28:121-30. 2012
    ..The objective of this study was to demonstrate the efficacy and safety of bilastine in patients with perennial allergic rhinitis (PAR)...
  52. ncbi Vandetanib for the treatment of thyroid cancer
    P B Langmuir
    AstraZeneca Pharmaceuticals, Wilmington, Delaware, USA
    Clin Pharmacol Ther 91:71-80. 2012
    ..This review discusses the development of vandetanib in patients with MTC and the benefits and risks in this patient population...
  53. ncbi Acute cannabinoid receptor type 1 (CB1R) modulation influences insulin sensitivity by an effect outside the central nervous system in mice
    D Song
    Department of Medicine, University of Toronto, Toronto, ON, Canada
    Diabetologia 54:1181-9. 2011
    ..Here we examined the relative contributions of acute CNS and extra-CNS CB1R modulation on insulin sensitivity using pharmacological gain- and loss-of-function of CB1R in mice...
  54. pmc A mouse model of high trait anxiety shows reduced heart rate variability that can be reversed by anxiolytic drug treatment
    Stefano Gaburro
    Department of Pharmacology and Toxicology, Institute of Pharmacy and Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria
    Int J Neuropsychopharmacol 14:1341-55. 2011
    ..These findings indicate that assessment of autonomic response in addition to freezing might be a useful indicator of the efficacy of novel anxiolytic treatments...
  55. ncbi Efficacy and safety of alogliptin added to pioglitazone in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label long-term extension study
    K Kaku
    Diabetes and Endocrine Division, Kawasaki Medical School, Okayama, Japan
    Diabetes Obes Metab 13:1028-35. 2011
    ..To assess the efficacy and safety of alogliptin added to pioglitazone versus pioglitazone monotherapy, in Japanese patients with type 2 diabetes who achieved inadequate glycaemic control on pioglitazone plus diet/exercise...
  56. ncbi Lowering of postprandial lipids in individuals with type 2 diabetes treated with alogliptin and/or pioglitazone: a randomised double-blind placebo-controlled study
    B Eliasson
    Department of Molecular and Clinical Medicine, University of Gothenburg, Goteborg, Sweden
    Diabetologia 55:915-25. 2012
    ..We assessed the effects of alogliptin (Alo) and Alo co-administered with pioglitazone (Pio) vs placebo (Pbo) on triacylglycerol (TG)-rich lipoproteins in type 2 diabetes before and following a high-fat meal...
  57. ncbi Efficacy and tolerability of the DPP-4 inhibitor alogliptin combined with pioglitazone, in metformin-treated patients with type 2 diabetes
    R A DeFronzo
    University of Texas Health Sciences Center, Diabetes Division, 7703 Floyd Curl Drive, San Antonio, Texas 78229, USA
    J Clin Endocrinol Metab 97:1615-22. 2012
    ..Optimal management of type 2 diabetes remains an elusive goal. Combination therapy addressing the core defects of impaired insulin secretion and insulin resistance shows promise in maintaining glycemic control...
  58. pmc The NAMPT inhibitor FK866 reverts the damage in spinal cord injury
    Emanuela Esposito
    Department of Clinical and Experimental Medicine and Pharmacology, School of Medicine, University of Messina, Torre Biologica Policlinico Universitario Via C, Valeria Gazzi, 98100 Messina, Italy
    J Neuroinflammation 9:66. 2012
    ..Given the role of inflammatory responses in spinal cord injury (SCI), the effect of NAMPT inhibitors was examined in this setting...
  59. pmc The role of sirtuin 2 activation by nicotinamide phosphoribosyltransferase in the aberrant proliferation and survival of myeloid leukemia cells
    Lan Dan
    Department of Molecular Hematopoiesis, Hannover Medical School, Carl Neuberg Str 1, 30625 Hannover, Germany
    Haematologica 97:551-9. 2012
    ..Inhibitors of nicotinamide phosphoribosyltransferase have recently been validated as therapeutic targets in leukemia, but the mechanism of leukemogenic transformation downstream of this enzyme is unclear...
  60. pmc Synergistic interactions between HDAC and sirtuin inhibitors in human leukemia cells
    Michele Cea
    Department of Internal Medicine, University of Genoa, Genoa, Italy
    PLoS ONE 6:e22739. 2011
    ..In conclusion, NAD(+)-independent HDACs and sirtuins cooperate in leukemia cells to avoid apoptosis. Combining sirtuin with HDAC inhibitors results in synergistic antileukemic activity that could be therapeutically exploited...
  61. ncbi Immunomodulatory and antitumor activity of Piper longum Linn. and piperine
    E S Sunila
    Amala Cancer Research Centre, Amalanagar, Thrissur 680 553, Kerala, India
    J Ethnopharmacol 90:339-46. 2004
    ..3%) and piperine (71.4%) on 5th day after immunization. Bone marrow cellularity and alpha-esterase positive cells were also increased by the administration of Piper longum extract and piperine...
  62. ncbi Vandetanib: first global approval
    Helen Commander
    RD Insight, Wolters Kluwer Pharma Solutions, Auckland, New Zealand
    Drugs 71:1355-65. 2011
    ..This article summarizes the milestones in the development of vandetanib leading to this first approval in malignant MTC...
  63. pmc Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse
    K J Jackson
    Department of Pharmacology and Toxicology, Medical Campus, Virginia Commonwealth University, Richmond, VA 23298, USA
    Psychopharmacology (Berl) 210:285-94. 2010
    ..Specifically, recent findings suggest that the kappa-opioid receptor (KOR) may play a role in aspects of nicotine dependence, which contribute to relapse and continued tobacco smoking...
  64. ncbi Induction of synaptic long-term potentiation after opioid withdrawal
    Ruth Drdla
    Department of Neurophysiology, Center for Brain Research, Medical University of Vienna, Spitalgasse 4, 1090 Vienna, Austria
    Science 325:207-10. 2009
    ..These findings provide a previously unrecognized target to selectively combat pro-nociceptive effects of opioids without compromising opioid analgesia...
  65. ncbi Piperine inhibits eosinophil infiltration and airway hyperresponsiveness by suppressing T cell activity and Th2 cytokine production in the ovalbumin-induced asthma model
    Seung Hyung Kim
    Institute of Traditional Medicine and Bioscience, Daejeon University, Daejeon, Republic of Korea
    J Pharm Pharmacol 61:353-9. 2009
    ....
  66. ncbi Effects of donepezil on activities of daily living: integrated analysis of patient data from studies in mild, moderate and severe Alzheimer's disease
    Serge Gauthier
    McGill Center for Studies in Aging, Douglas Mental Health University Institute, Douglas Hospital, Verdun, QC, Canada
    Int Psychogeriatr 22:973-83. 2010
    ....
  67. pmc Cholinergic enhancement reduces spatial spread of visual responses in human early visual cortex
    Michael A Silver
    School of Optometry, University of California, Berkeley, Berkeley, CA 94720, USA
    Neuron 60:904-14. 2008
    ..These findings demonstrate that acetylcholine regulates spatial integration in human visual cortex...
  68. ncbi Interaction between cannabinoid compounds and diazepam on anxiety-like behaviour of mice
    Nima Naderi
    Neuroscience Research Center, Shaheed Beheshti University Medical Sciences, PO Box 19615 1178, Tehran, Iran
    Pharmacol Biochem Behav 89:64-75. 2008
    ..Moreover, it has been shown that enhancement of the function of endocannabinoids could increase the anxiolytic effect of diazepam...
  69. ncbi Effect of the cholinesterase inhibitor donepezil on cardiac remodeling and autonomic balance in rats with heart failure
    Yoshihisa Okazaki
    Department of Artificial Organ Medicine, Division of Surgical Medicine, Osaka University Graduate School of Medicine, 2 2 Yamadaoka, Suita, Osaka 565 0871, Japan
    J Physiol Sci 60:67-74. 2010
    ..These findings indicated that donepezil reproduced the anti-remodeling effect of electrical vagal stimulation. Further studies are warranted to evaluate the clinical usefulness of donepezil in heart failure...
  70. pmc Donepezil improves episodic memory in young individuals vulnerable to the effects of sleep deprivation
    Lisa Y M Chuah
    Cognitive Neuroscience Laboratory, Duke NUS Graduate Medical School, Singapore
    Sleep 32:999-1010. 2009
    ..We investigated if donepezil, a long-acting orally administered cholinesterase inhibitor, would reduce episodic memory deficits associated with 24 h of sleep deprivation...
  71. ncbi Chronic psychoemotional stress impairs cannabinoid-receptor-mediated control of GABA transmission in the striatum
    Silvia Rossi
    Clinica Neurologica, Dipartimento di Neuroscienze, Universita Tor Vergata, 00133 Rome, Italy
    J Neurosci 28:7284-92. 2008
    ..Targeting cannabinoid CB(1) receptors or endocannabinoid metabolism might be a valuable option to treat stress-associated neuropsychiatric conditions...
  72. ncbi Halofuginone inhibits Smad3 phosphorylation via the PI3K/Akt and MAPK/ERK pathways in muscle cells: effect on myotube fusion
    Suzy Roffe
    Department of Animal Sciences, The Hebrew University of Jerusalem, PO Box 12, Rehovot 76100, Israel
    Exp Cell Res 316:1061-9. 2010
    ..Together, the data suggest a role, either direct or via inhibition of Smad3 phosphorylation, for Akt or MAPK/ERK in halofuginone-enhanced myotube fusion, a feature which is crucial to improving muscle function in muscular dystrophies...
  73. pmc Receptors and channels targeted by synthetic cannabinoid receptor agonists and antagonists
    R G Pertwee
    Institute of Medical Sciences, University of Aberdeen, Foresterhill, Scotland, UK
    Curr Med Chem 17:1360-81. 2010
    ..It begins with a brief description of how each of these ligands interacts with CB(1) and/or CB(2) receptors...
  74. ncbi CCR5 blockade in rheumatoid arthritis: a randomised, double-blind, placebo-controlled clinical trial
    Arno W R van Kuijk
    Academic Medical Center University of Amsterdam, The Netherlands
    Ann Rheum Dis 69:2013-6. 2010
    ..The rationale for testing CCR5 blockade in patients with RA was supported by the effects of a CCR5 antagonist in collagen-induced arthritis in rhesus monkeys. The effects of CCR5 blockade in patients with active RA were explored...
  75. ncbi Rapid development of tolerance to analgesia during remifentanil infusion in humans
    H R Vinik
    Department of Anesthesiology, University of Alabama at Birmingham, USA
    Anesth Analg 86:1307-11. 1998
    ..We conclude that the development of tolerance should be included in the calculations for target-controlled infusions...
  76. ncbi Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors
    Chiyoko Sekine
    Clinical Immunology, RIKEN Research Center of Allergy and Immunology, Yokohama, Japan
    J Immunol 180:1954-61. 2008
    ..Thus, the two small-molecule CDK inhibitors ameliorated arthritis models in a distinctive way, compared with other immunosuppressive drugs...
  77. ncbi Amphetamine decreases behavioral inhibition by stimulation of dopamine D2, but not D3, receptors
    Marcel M van Gaalen
    Neuroscience Research, GPRD, Abbott, Knollstrasse, Ludwigshafen, Germany
    Behav Pharmacol 20:484-91. 2009
    ..The effect of amphetamine was attenuated by L-741,626 (3 mg/kg), whereas SB-277011 (3 mg/kg) had no effect. Therefore, amphetamine-induced behavioral disinhibition depends on D(2), but not D(3), receptor stimulation...
  78. ncbi Effects of donepezil on verbal memory after semantic processing in healthy older adults
    David B Fitzgerald
    Department of Neurology, University of Florida, Jacksonville, FL 32610 0236, USA
    Cogn Behav Neurol 21:57-64. 2008
    ..To learn if acetylcholinesterase inhibitors alter verbal recall by improving semantic encoding in a double-blind randomized placebo-controlled trial...
  79. ncbi A randomized, double-blind, placebo-controlled phase II study of vandetanib plus docetaxel/prednisolone in patients with hormone-refractory prostate cancer
    Jozsef Horti
    National Institute of Oncology, Budapest, Hungary
    Cancer Biother Radiopharm 24:175-80. 2009
    ..2%), erythematous rash (14% vs. 2%), and exfoliative rash (12% vs. 2%). In this study of patients with mHRPC, vandetanib + DP did not demonstrate any efficacy benefit, compared with placebo + DP...
  80. ncbi Donepezil treatment of patients with severe Alzheimer's disease in a Japanese population: results from a 24-week, double-blind, placebo-controlled, randomized trial
    Akira Homma
    Dementia Interventional Research Group, Tokyo Metropolitan Institute of Gerontology, Tokyo, Japan
    Dement Geriatr Cogn Disord 25:399-407. 2008
    ..A 24-week, randomized, parallel-group, double-blind placebo-controlled study was conducted to evaluate the efficacy and tolerability of donepezil in severe Alzheimer's disease (AD)...
  81. ncbi Long-term effect of CB1 blockade with rimonabant on cardiometabolic risk factors: two year results from the RIO-Europe Study
    Luc F Van Gaal
    Department of Diabetology, Metabolism, and Clinical Nutrition, Antwerp University Hospital, Wilrijkstraat 10, B 2650 Edegem Antwerp, Belgium
    Eur Heart J 29:1761-71. 2008
    ..We report the 2 year efficacy and tolerability data of rimonabant...
  82. ncbi Reduced anxiety-like behaviour induced by genetic and pharmacological inhibition of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) is mediated by CB1 receptors
    Fabricio A Moreira
    Department of Physiological Chemistry, Johannes Gutenberg University Mainz, Duesbergweg 6, D 55099 Mainz, Germany
    Neuropharmacology 54:141-50. 2008
    ..In addition, it indicates an increased activation of CB1 receptors as a mechanism underlying the effects of FAAH inhibition in two models of anxiety...
  83. 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...
  84. ncbi Functional interaction between opioid and cannabinoid receptors in drug self-administration
    M Navarro
    Departamentos de Psicobiologia and Fisiologia, Universidad Complutense de Madrid, 28223 Madrid, Spain
    J Neurosci 21:5344-50. 2001
    ..The present results show the existence of a cross-interaction between opioid and cannabinoid systems in behavioral responses related to addiction and open new strategies for the treatment of opiate dependence...
  85. ncbi Vandetanib in locally advanced or metastatic differentiated thyroid cancer: a randomised, double-blind, phase 2 trial
    Sophie Leboulleux
    Institut Gustave Roussy, Universite Paris Sud, Villejuif, France
    Lancet Oncol 13:897-905. 2012
    ..We aimed to assess efficacy and safety of vandetanib, a tyrosine kinase inhibitor of RET, VEGFR and EGFR signalling, in this setting...
  86. ncbi Potential modulation of plasma ghrelin and glucagon-like peptide-1 by anorexigenic cannabinoid compounds, SR141716A (rimonabant) and oleoylethanolamide
    Patrice D Cani
    Unité de Pharmacocinétique, Metabolisme, Nutrition et Toxicologie, Ecole de Pharmacie, Universite Catholique de Louvain, Brussels, Belgium
    Br J Nutr 92:757-61. 2004
    ....
  87. ncbi Potent antitumor effects of ZD6474 on neuroblastoma via dual targeting of tumor cells and tumor endothelium
    Paul Beaudry
    Department of Vascular Biology, Boston Children s Hospital, Boston, Massachusetts, USA
    Mol Cancer Ther 7:418-24. 2008
    ..In conclusion, dual targeting of tumor cells, potentially through RET inhibition, and tumor vasculature with ZD6474 leads to potent antitumor effects. This approach merits further investigation for patients with neuroblastoma...
  88. ncbi Comparison of peripheral and central effects of single and repeated oral dose administrations of bilastine, a new H1 antihistamine: a dose-range study in healthy volunteers with hydroxyzine and placebo as control treatments
    Consuelo García-Gea
    Centre d Investigacio de Medicaments, Institut de Recerca, Servei de Farmacologia Clinica, Hospital de la Santa Creu i Sant Pau, Barcelona, Spain
    J Clin Psychopharmacol 28:675-85. 2008
    ..The 40-mg dose of BIL produced subjective report of sedation, whereas unwanted objective CNS side effects were observed only with the 80-mg dose...
  89. ncbi D-serine augments NMDA-NR2B receptor-dependent hippocampal long-term depression and spatial reversal learning
    Steven Duffy
    Samuel Lunenfeld Research Institute, Mount Sinai Hospital, Toronto, ON, Canada
    Neuropsychopharmacology 33:1004-18. 2008
    ..By enhancing this form of synaptic plasticity, D-serine could improve cognitive flexibility in psychiatric disorders characterized by perseveration of aberrant ideation or behaviors...
  90. ncbi Nampt/PBEF/visfatin and cancer
    Tie qiang Bi
    Department of General Surgery, The First Affiliated Hospital, Medical School of Xi an Jiaotong University, Xi an, Shaanxi, China
    Cancer Biol Ther 10:119-25. 2010
    ..This review will focus on its role in carcinogenesis and cancer progression and its inhibitors as therapeutic target for cancer treatment...
  91. pmc Curcuminoids inhibit multiple human cytochromes P450, UDP-glucuronosyltransferase, and sulfotransferase enzymes, whereas piperine is a relatively selective CYP3A4 inhibitor
    Laurie P Volak
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    Drug Metab Dispos 36:1594-605. 2008
    ..Based on these data and expected tissue concentrations of inhibitors, we predict that a p.o. administered curcuminoid/piperine combination is most likely to inhibit CYP3A, CYP2C9, UGT, and SULT metabolism within the intestinal mucosa...
  92. ncbi Inhibition of in vitro enteric neuronal development by endothelin-3: mediation by endothelin B receptors
    J J Wu
    Department of Anatomy and Cell Biology and Center for Neurobiology and Behavior, College of Physicians and Surgeons, Columbia University, New York, New York, USA
    Development 126:1161-73. 1999
    ....
  93. 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...
  94. ncbi Dopamine modulation of state-dependent endocannabinoid release and long-term depression in the striatum
    Anatol C Kreitzer
    Department of Psychiatry and Behavioral Sciences, Stanford University Medical School, Palo Alto, California 94305, USA
    J Neurosci 25:10537-45. 2005
    ..However, this gating of plasticity by dopamine is accomplished via an unexpected mechanism involving the regulation of mGluR-dependent endocannabinoid release...
  95. ncbi A preclinical study on the rescue of normal tissue by nicotinic acid in high-dose treatment with APO866, a specific nicotinamide phosphoribosyltransferase inhibitor
    Uffe Høgh Olesen
    Experimental Pathology Unit, Rigshospitalet 3733, Biocenter, Ole Maaloes Vej 5, Copenhagen, Denmark
    Mol Cancer Ther 9:1609-17. 2010
    ..In conclusion, the combination of high doses of APO866 with rescue by nicotinic acid may significantly increase the therapeutic potential in a subset of cancers with low expression of nicotinic acid phosphoribosyltransferase...
  96. ncbi Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, in murine renal cell carcinoma
    Joachim Drevs
    Department of Medical Oncology, Tumor Biology Center, Breisacher Strasse 117, D 79106 Freiburg, Federal Republic of Germany
    Anticancer Res 23:4853-8. 2003
    ..FK-866 has antitumoral and antimetastatic activity in RENCA mice. Furthermore, this is the first report to describe a strong antiangiogenic potency of FK-866...
  97. ncbi Long-term outcome and prediction models of activities of daily living in Alzheimer disease with cholinesterase inhibitor treatment
    Carina Wattmo
    Department of Clinical Sciences, Clinical Memory Research Unit, Malmo, Lund University, Sweden
    Alzheimer Dis Assoc Disord 25:63-72. 2011
    ..AD severity at baseline is a key factor in obtaining reliable clinical prognoses of the long-term ADL ability. The dosage of ChEI treatment could possibly lead to a different functional outcome...
  98. pmc Tyrosine phosphorylation of the N-Methyl-D-Aspartate receptor 2B subunit in spinal cord contributes to remifentanil-induced postoperative hyperalgesia: the preventive effect of ketamine
    Xiaoping Gu
    Department of Anesthesiology, Drum Tower Hospital, Medical Department of Nanjing University, Nanjing 210008, Jiangsu Province, China
    Mol Pain 5:76. 2009
    ....
  99. ncbi Anti-Alzheimer's drug, donepezil, markedly improves long-term survival after chronic heart failure in mice
    Takemi Handa
    Department of Cardiovascular Control, Kochi Medical School, Nankoku, Japan
    J Card Fail 15:805-11. 2009
    ....
  100. ncbi The cannabinoid CB1 receptor mediates retrograde signals for depolarization-induced suppression of inhibition in cerebellar Purkinje cells
    Takayuki Yoshida
    Department of Cellular Neurophysiology, Graduate School of Medical Science, Kanazawa University, Kanazawa 920 8640, Japan
    J Neurosci 22:1690-7. 2002
    ..These results clearly indicate that the CB1 receptor mediates retrograde signal for DSI in cerebellar Purkinje cells...
  101. ncbi Remifentanil-induced postoperative hyperalgesia and its prevention with small-dose ketamine
    Vincent Joly
    Department of Anesthesia, Institut National de la Santé et de la Recherche Médicale INSERM E 332, Hopital Ambroise Pare, Assistance Publique Hopitaux de Paris, France
    Anesthesiology 103:147-55. 2005
    ....

Research Grants65

  1. Alkaloid Synthesis via Asymmetric C-CN Activation
    Christopher J Douglas; Fiscal Year: 2013
    ..last few years, our laboratory discovered that important structural motifs in medicinal alkaloids, indoles and piperidines, could be synthesized with extraordinary ease using highly unusual reactivity...
  2. Metal-Catalyzed Cross Coupling with N,O-Acetals and Acetals
    ABIGAIL GUTMANN DOYLE; Fiscal Year: 2013
    ..The substituted dihydroquinolines, piperidines, chromenes, and pyrans that we will obtain from these studies constitute the core structural elements of small ..
  3. MECHANISM OF ACTION OF FIRE ANT VENOM
    NANCY LIND; Fiscal Year: 1980
    ..the antimicrobial activity of the venom is also due to membrane disruption, to synthesize additional venom piperidines and related compounds and study their structure-activity relations for histamine- and LDH-release from mast ..
  4. A Flexible and Concise Approach to the Citrinadins: Total Synthesis of Citrinadin
    DEVON ALLEN MUNDAL; Fiscal Year: 2012
    ..proposed synthetic route to the citrinadins will capitalize on the use of methoxypyridines as surrogates for piperidines in the synthesis of complex alkaloids...
  5. ROUTES TO CHIRAL CARBOCYCLIC AND HETEROCYCLIC COMPOUNDS
    A Meyers; Fiscal Year: 2000
    ..request we will describe chemistry which will access a number of important classes of chiral heterocycles (piperidines, pyrrolidines, azepines) as well as multifunctional carbocycles whose architecture quickly suggest they can be ..
  6. Asymmetric Synthesis of Nitrogen Heterocycles
    Tomislav Rovis; Fiscal Year: 2013
    ..2+2+2] cycloadditions;2) Investigate the oxidative coupling of amides and alkene/alkyne ? systems to assemble piperidines by a catalyzed/oxidative protocol;3) Exploit readily available aza-dienes in metal-catalyzed [4+2] reactions;..
  7. METHODS APPLICABLE TO B-LACTAM AND ALKALOID SYNTHESES
    HARRY WASSERMAN; Fiscal Year: 1991
    ..are to develop new chemistry for the synthesis of beta-lactams, functionalized pyrrolidines and substituted piperidines which will have applicability in the formation of beta-lactam antibiotics and alkaloids...
  8. Tandem Cycloaddition Chemistry of 2-Azoniaheterodienes
    SCOTT DENMARK; Fiscal Year: 2007
    ..These hybrid heterodiene/dipoles offer great potential for the general synthesis of piperidines and piperidine-embedded polycyclic compounds...
  9. NOVEL APPROACHES TO ALKALOID SYNTHESIS
    Patrick Mariano; Fiscal Year: 2004
    ..Prins cyclizations have been demonstrated by applications to stereocontrolled preparation of polyhydroxylated-piperidines and tetrahydro-pyrans and -furans...
  10. Mo-Catalyzed Enantioselective Synthesis of Heterocycles
    GERMAN CORTEZ; Fiscal Year: 2005
    ..utility of Mo-catalyzed Asymmetric Ring- Opening Cross-Metathesis (AROCM) in the synthesis of chiral pyrans and piperidines, two structural motifs present in myriad biologically important natural products...
  11. BEHAVIORAL EVALUATION OF NOVEL DAT ANTAGONIST
    MONIKA TRZCINSKA; Fiscal Year: 2000
    ..examined are the diphenylmethoxypiperazines (specific GBR analogs; the Nocaine-A series) that are partial cocaine agonists and a series of disubstituted piperidines (the Nocaine-B series). PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE
  12. Halopiperidines for imaging of monoamine transporters
    MILES SMITH; Fiscal Year: 2003
    ..Herein, we propose the rational design and synthesis a series of halogenated piperidines as potential radio-tracers for imaging of the monoamine transporters utilizing PET and SPECT...
  13. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..these new ([unreadable]-amino ketones will be employed in syntheses of toxic frog skin polysubstituted piperidines not previously prepared...
  14. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....
  15. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  16. CB1 Receptors: Cocaine Reinforcement and Relapse
    Sara Ward; Fiscal Year: 2007
    ..The second goal is to employ this set of procedures to assess the role of the CB1 receptor system in cocaine's reinforcing effects and relapse to cocaine seeking. ..
  17. Developmental Psychopharmacology of Antipsychotics
    JENNY WILEY; Fiscal Year: 2007
    ..This information will help to provide a more rational basis for making treatment decisions concerning children and adolescents who may benefit from treatment with an antipsychotic. [unreadable] [unreadable]..
  18. "Post-partum steroid withdrawal-induced depression"
    REBECCA CRAFT; Fiscal Year: 2006
    ..Findings from the proposed model will enhance our understanding of the etiology of PPD and possibly lead to improved treatment options. ..
  19. Opiate-Induced Tolerance & Hyperalgesia in Pain Patients
    Lawrence Chu; Fiscal Year: 2008
    ..abstract_text> ..
  20. Development of Natural Product as Antimalarial Agent
    Shuren Zhu; Fiscal Year: 2007
    ..Investigational new drug (IND) application will then be filed with FDA. [unreadable] [unreadable] [unreadable]..
  21. Pre-Clinical Development of Natural Product Analogues as Antimalarial Agents
    Shuren Zhu; Fiscal Year: 2007
    ..Investigational new drug (IND) application will then be filed with FDA. Radix Pharmaceuticals has strategic alliance with commercial partners for Phase III development. [unreadable] [unreadable] [unreadable]..
  22. 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. ..
  23. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  24. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  25. Pharmacotherapy of Cannabinoid Withdrawal: Pre-Clinical Studies
    Lance R McMahon; Fiscal Year: 2010
    ..Collectively, these specific aims provide a framework for developing novel pharmacotherapies of marijuana withdrawal that could markedly decrease marijuana use and dependence. ..
  26. Drug discrimination and THC withdrawal in monkeys
    LANCE MCMAHON; Fiscal Year: 2005
    ..abstract_text> ..
  27. PET Imaging of the Pancreas in Murine Models of Diabetes
    Paige Clark; Fiscal Year: 2005
    ..The method could also be useful in evaluating the function of pancreatic transplants and successful engraftment of transplanted progenitor or beta cells. ..
  28. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
    ..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
  29. Pharmacoresistance in rats with kainate-induced epilepsy
    F Dudek; Fiscal Year: 2005
    ..abstract_text> ..
  30. Siblings With Ischemic Stroke Study (SWISS)
    JAMES MESCHIA; Fiscal Year: 2009
    ..DNA banking and the creation of permanent lymphoblastoid cell lines will be done to permit future collaborative efforts to study the genetic basis for stroke risk. ..
  31. Abused Inhalant Actions at GABA and Glutamate Synapses
    M MacIver; Fiscal Year: 2008
    ..Taken together, the results will allow a quantitative comparison of drug effects on glutamate and GABA-mediated transmission for commonly abused solvents including: toluene, 1,1,1-trichloroethane andtrichloroethylene. ..
  32. Contributions of sleep/rhythms/fatigue to "chemobrain"
    Sonia Ancoli Israel; Fiscal Year: 2009
    ..The reported phenomena of chemobrain will be examined to see if it is related to the complaint of fatigue or sleep disruptions, both of which are known to contribute to decreases in cognitive functioning. ..
  33. New PET Radiotracers-Monoamine Transporters
    Michael Kilbourn; Fiscal Year: 2003
    ....
  34. Dedicated High Performance Human Brain/Preclinical PET
    DEAN WONG; Fiscal Year: 2004
    ..abstract_text> ..
  35. Prenatal Cannabis Effect on the Endocannabinoid System
    VINOD YARAGUDRI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  36. Folic Acid and B Vitamins to Prevent Fracture in Women
    Steven Cummings; Fiscal Year: 2009
    ..The proposed study is a cost-effective approach to determining whether a safe and inexpensive nutritional intervention substantially reduces the risk of fracture and to understanding the mechanism of this effect. ..
  37. Interferon Regulation in Systemic Lupus
    Lionel B Ivashkiv; Fiscal Year: 2010
    ..These experiments will yield insight into the molecular pathogenesis of SLE and identify novel therapeutic approaches to manipulatecytokine activity in SLE at the level of signal transduction. ..
  38. NEUROPHARMACOLOGY OF PRIMATE COGNITION
    MICHAEL TAFFE; Fiscal Year: 2002
    ..abstract_text> ..
  39. NEUROBEHAVIORAL PHARMACOLOGY OF STIMULANTS
    Kathryn A Cunningham; Fiscal Year: 2010
    ....
  40. TRANSPLANT IMMUNOLOGY OF IL2 IFNY DOUBLE KNOCKOUT MICE
    Martin Zand; Fiscal Year: 2002
    ..In contrast, if the DKO mice are tolerant to islet allografts, we will determine the mechanism by adoptive transfer of tolerance inducing T lymphocyte subsets. ..
  41. Cytokine induction of Claudin-1 in epicardial border zone of ischemic heart
    Heather S Duffy; Fiscal Year: 2010
    ..We also propose to use sophisticated computer modeling to assess the impact on propagation that the addition of these extracellular barriers would provide. ..
  42. Agilent 5973 GC/MS System
    GARY MOLANDER; Fiscal Year: 2002
    ..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
  43. 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. ..
  44. Synthesis and Evaluation of Sigma-Active Cocaine Antagonists
    Rae R Matsumoto; Fiscal Year: 2010
    ..It is anticipated that the results of this project will stimulate the rational development of new a2 receptor probes and ultimately contribute to improved treatments for psychostimulant abuse. ..
  45. Gene Expression in Prediabetes: Potential Role of PGC-1
    MARY PATTI; Fiscal Year: 2006
    ..abstract_text> ..
  46. 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]..
  47. Progression of temporal lobe epilepsy
    F Edward Dudek; Fiscal Year: 2007
    ..abstract_text> ..
  48. Flavopiridol Targets Transcription Factor/DNA Complexes
    Keith Bible; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  49. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  50. Catalytic Processes for Selective Organic Synthesis
    GARY MOLANDER; Fiscal Year: 2005
    ..4) Carbometalation/cyclization reactions will be explored utilizing organochromium species. 5) Ligands and catalytic systems designed for asymmetric synthesis will be explored. ..
  51. FATIGUE, SLEEP AND CIRCADIAN RHYTHMS IN BREAST CANCER
    Sonia Ancoli Israel; Fiscal Year: 2004
    ..Results will provide a scientific basis for future intervention studies, particularly studies with light therapy which can re-synchronize rhythms. ..
  52. Coactivation of Estrogen Receptor alpha/Sp1
    Stephen Safe; Fiscal Year: 2006
    ..abstract_text> ..
  53. Predictors of Alzheimers Disease in Mild Cognitive Impairment
    Oscar Lopez; Fiscal Year: 2007
    ..g., structural and perfusion MRI, plasma beta-amyloid) and the factors that modify the risk to express the clinical syndrome takes on an added importance. [unreadable] [unreadable] [unreadable] [unreadable]..
  54. DEVELOPING AND IMPROVING INSTITUTIONAL ANIMAL RESOURCES
    JANICE WAGNER; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  55. Air Pollution Exposure/Atherosclerosis:Vascular Mechanism
    Sanjay Rajagopalan; Fiscal Year: 2007
    ..This study is expected to provide a firm linkage between CAPS exposure and atherosclerosis progression and will provide a pathophysiologic basis for the adverse cardiovascular effects of CAPS. ..
  56. SIV Behavioral Pathology: Manipulation of Viral Load
    MICHAEL TAFFE; Fiscal Year: 2004
    ..abstract_text> ..
  57. Caregiver-based Intervention for Persistent Delirium
    Edward Marcantonio; Fiscal Year: 2007
    ..If promising, our findings will serve as pilot data for a definitive trial to test this novel strategy to improve the health of a vulnerable population of elders and their caregivers. [unreadable] [unreadable] [unreadable]..
  58. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..chemistry will contribute significantly to the synthesis of highly substituted pyrrolidines, piperidines, and their bicyclic analogs (i.e., pyrrolizidines, indolizidines, and quinolizidines)...
  59. Restraint stress-induced neurogenic bladder inflammation
    Theoharis Theoharides; Fiscal Year: 2006
    ..Our findings may be relevant to the pathophysiology of IC and may suggest new therapeutic approaches. ..
  60. IMAGING DOPAMINE RELEASE/ENDOCRINE CHANGES IN ALCOHOLISM
    DEAN WONG; Fiscal Year: 2004
    ..If the initial D2 receptor deficits are exacerbated by alcohol abuse one can envision a positive feedback loop hard to break. ..
  61. Axonal Sprouting of GABAergic Neurons in Epileptogenesis
    SUZANNE BAUSCH; Fiscal Year: 2004
    ..abstract_text> ..
  62. CORTICOTROPIN RELEASING HORMONE INDUCED DURA MAST CELL A
    Theoharis Theoharides; Fiscal Year: 2001
    ..They may also help explain some key events in the pathophysiology of migraines, the clinical symptoms of which are often precipitated by stress. ..
  63. Mast cells, antidepressants and chronic fatigue syndrome
    Theoharis Theoharides; Fiscal Year: 2007
    ..Future studies will build on these findings to develop in vitro and in vivo models of CFS and lead to clinical trials with select antidepressants or other molecules that inhibit brain mast cells. [unreadable] [unreadable] [unreadable]..