benzylamines

Summary

Summary: Toluenes in which one hydrogen of the methyl group is substituted by an amino group. Permitted are any substituents on the benzene ring or the amino group.

Top Publications

  1. ncbi Stroke prevention with the oral direct thrombin inhibitor ximelagatran compared with warfarin in patients with non-valvular atrial fibrillation (SPORTIF III): randomised controlled trial
    S Bertil Olsson
    Department of Cardiology, University Hospital, Lund SE 221 85, Sweden
    Lancet 362:1691-8. 2003
  2. ncbi 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo
    E P Garvey
    Institute of Biochemistry, Glaxo Wellcome, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 272:4959-63. 1997
  3. ncbi Ca2+/calmodulin-dependent protein kinase modulates cardiac ryanodine receptor phosphorylation and sarcoplasmic reticulum Ca2+ leak in heart failure
    Xun Ai
    Department of Medicine, University of Illinois at Chicago, IL 60612, USA
    Circ Res 97:1314-22. 2005
  4. ncbi Secondary prevention of venous thromboembolism with the oral direct thrombin inhibitor ximelagatran
    Sam Schulman
    Coagulation Unit, Department of Medicine, Karolinska Hospital, Stockholm, Sweden
    N Engl J Med 349:1713-21. 2003
  5. ncbi miR-1 overexpression enhances Ca(2+) release and promotes cardiac arrhythmogenesis by targeting PP2A regulatory subunit B56alpha and causing CaMKII-dependent hyperphosphorylation of RyR2
    Dmitry Terentyev
    Davis Heart and Lung Research Institute, Department of Physiology and Cell Biology, Ohio State University, Columbus, OH 43210, USA
    Circ Res 104:514-21. 2009
  6. ncbi Oral ximelagatran for secondary prophylaxis after myocardial infarction: the ESTEEM randomised controlled trial
    Lars Wallentin
    Uppsala Clinical Research Centre, University Hospital, Uppsala, Sweden
    Lancet 362:789-97. 2003
  7. pmc ApoE promotes the proteolytic degradation of Abeta
    Qingguang Jiang
    Alzheimer Research Laboratory, Department of Neurosciences, Case Western Reserve University School of Medicine, Cleveland, OH 44106, USA
    Neuron 58:681-93. 2008
  8. ncbi Death, cardiac dysfunction, and arrhythmias are increased by calmodulin kinase II in calcineurin cardiomyopathy
    Michelle S C Khoo
    Department of Medicine, Vanderbilt University, Nashville, Tenn, USA
    Circulation 114:1352-9. 2006
  9. ncbi Calmodulin kinase II inhibition prevents arrhythmias in RyR2(R4496C+/-) mice with catecholaminergic polymorphic ventricular tachycardia
    Nian Liu
    Cardiovascular Genetics Program, The Leon H Charney Division of Cardiology, New York University School of Medicine, New York, USA
    J Mol Cell Cardiol 50:214-22. 2011
  10. ncbi Rapid and sensitive kinetic assay for characterization of omega-transaminases
    Sebastian Schätzle
    Institute of Biochemistry, Department of Biotechnology and Enzyme Catalysis, Greifswald University, Felix Hausdorff Str 4, 17487 Greifswald, Germany
    Anal Chem 81:8244-8. 2009

Research Grants

Detail Information

Publications231 found, 100 shown here

  1. ncbi Stroke prevention with the oral direct thrombin inhibitor ximelagatran compared with warfarin in patients with non-valvular atrial fibrillation (SPORTIF III): randomised controlled trial
    S Bertil Olsson
    Department of Cardiology, University Hospital, Lund SE 221 85, Sweden
    Lancet 362:1691-8. 2003
    ..The oral direct thrombin inhibitor ximelagatran represents a potential alternative. We aimed to establish whether ximelagatran is non-inferior to warfarin, within a margin of 2% per year, for prevention of stroke and systemic embolism...
  2. ncbi 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo
    E P Garvey
    Institute of Biochemistry, Glaxo Wellcome, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 272:4959-63. 1997
    ..Thus, the potency and selectivity of 1400W inhibition of iNOS both in vitro and in vivo were far greater than of any previously described iNOS inhibitor...
  3. ncbi Ca2+/calmodulin-dependent protein kinase modulates cardiac ryanodine receptor phosphorylation and sarcoplasmic reticulum Ca2+ leak in heart failure
    Xun Ai
    Department of Medicine, University of Illinois at Chicago, IL 60612, USA
    Circ Res 97:1314-22. 2005
    ..Our results suggest that CaMKII-dependent phosphorylation of RyR2 is involved in enhanced SR diastolic Ca leak and reduced SR Ca load in HF, and may thus contribute to arrhythmias and contractile dysfunction in HF...
  4. ncbi Secondary prevention of venous thromboembolism with the oral direct thrombin inhibitor ximelagatran
    Sam Schulman
    Coagulation Unit, Department of Medicine, Karolinska Hospital, Stockholm, Sweden
    N Engl J Med 349:1713-21. 2003
    ..For many patients with venous thromboembolism, secondary prevention with vitamin K antagonists is not extended beyond six months, since the risk of recurrence may be outweighed by the risk of major bleeding...
  5. ncbi miR-1 overexpression enhances Ca(2+) release and promotes cardiac arrhythmogenesis by targeting PP2A regulatory subunit B56alpha and causing CaMKII-dependent hyperphosphorylation of RyR2
    Dmitry Terentyev
    Davis Heart and Lung Research Institute, Department of Physiology and Cell Biology, Ohio State University, Columbus, OH 43210, USA
    Circ Res 104:514-21. 2009
    ..We conclude that miR-1 enhances cardiac excitation-contraction coupling by selectively increasing phosphorylation of the L-type and RyR2 channels via disrupting localization of PP2A activity to these channels...
  6. ncbi Oral ximelagatran for secondary prophylaxis after myocardial infarction: the ESTEEM randomised controlled trial
    Lars Wallentin
    Uppsala Clinical Research Centre, University Hospital, Uppsala, Sweden
    Lancet 362:789-97. 2003
    ..We aimed to assess the effectiveness of ximelagatran and acetylsalicylic acid for prevention of death, non-fatal myocardial infarction, and severe recurrent ischaemia after a recent myocardial infarction...
  7. pmc ApoE promotes the proteolytic degradation of Abeta
    Qingguang Jiang
    Alzheimer Research Laboratory, Department of Neurosciences, Case Western Reserve University School of Medicine, Cleveland, OH 44106, USA
    Neuron 58:681-93. 2008
    ..GW3965 treatment also reversed contextual memory deficits. These data demonstrate a mechanism through which ApoE facilitates the clearance of Abeta from the brain and suggest that LXR agonists may represent a novel therapy for AD...
  8. ncbi Death, cardiac dysfunction, and arrhythmias are increased by calmodulin kinase II in calcineurin cardiomyopathy
    Michelle S C Khoo
    Department of Medicine, Vanderbilt University, Nashville, Tenn, USA
    Circulation 114:1352-9. 2006
    ....
  9. ncbi Calmodulin kinase II inhibition prevents arrhythmias in RyR2(R4496C+/-) mice with catecholaminergic polymorphic ventricular tachycardia
    Nian Liu
    Cardiovascular Genetics Program, The Leon H Charney Division of Cardiology, New York University School of Medicine, New York, USA
    J Mol Cell Cardiol 50:214-22. 2011
    ..CaMKII inhibition may therefore represent a novel therapeutic target for patients with CPVT...
  10. ncbi Rapid and sensitive kinetic assay for characterization of omega-transaminases
    Sebastian Schätzle
    Institute of Biochemistry, Department of Biotechnology and Enzyme Catalysis, Greifswald University, Felix Hausdorff Str 4, 17487 Greifswald, Germany
    Anal Chem 81:8244-8. 2009
    ..This method was used for the characterization of a novel omega-TA cloned from Rhodobacter sphaeroides, and the data obtained were in excellent accordance with a standard capillary electrophoresis assay...
  11. pmc Ser-2030, but not Ser-2808, is the major phosphorylation site in cardiac ryanodine receptors responding to protein kinase A activation upon beta-adrenergic stimulation in normal and failing hearts
    Bailong Xiao
    Cardiovascular Research Group, Department of Physiology and Biophysics, University of Calgary, Calgary, Alberta, Canada
    Biochem J 396:7-16. 2006
    ..Our results also suggest that phosphorylation of RyR2 at Ser-2030 may be an important event associated with altered Ca2+ handling and cardiac arrhythmia that is commonly observed in heart failure upon beta-adrenergic stimulation...
  12. pmc Effective post-insult neuroprotection by a novel Ca(2+)/ calmodulin-dependent protein kinase II (CaMKII) inhibitor
    Rebekah S Vest
    Department of Pharmacology, University of Colorado Denver School of Medicine, Aurora, CO 80045, USA
    J Biol Chem 285:20675-82. 2010
    ..Together, these data demonstrate that inhibition of autonomous CaMKII activity provides a promising therapeutic avenue for post-insult neuro-protection after stroke...
  13. ncbi Norepinephrine regulates locomotor hyperactivity in the mouse mutant coloboma
    Michelle D Jones
    Department of Neurology, Johns Hopkins University School of Medicine, Meyer 6 181, 600 North Wolfe Street, Baltimore, MD 21287, USA
    Pharmacol Biochem Behav 75:209-16. 2003
    ..These results suggest that NE regulation in the CNS plays an important role in the expression of hyperactivity in this mouse model, consistent with results of human studies and current models of ADHD...
  14. ncbi Visualization of synaptic Ca2+ /calmodulin-dependent protein kinase II activity in living neurons
    Keizo Takao
    RIKEN Massachusetts Institute of Technology MIT Neuroscience Research Center, The Picower Center for Learning and Memory, Department of Brain and Cognitive Sciences, MIT, Cambridge, Massachusetts 02139, USA
    J Neurosci 25:3107-12. 2005
    ..In combination with two-photon microscopy, we demonstrate that Camuialpha can be used to observe temporal and spatial regulation of CaMKII activity in living neurons...
  15. pmc Palladium- and copper-catalyzed arylation of carbon-hydrogen bonds
    OLAFS DAUGULIS
    Department of Chemistry, University of Houston, Houston, Texas 77204 5003, USA
    Acc Chem Res 42:1074-86. 2009
    ..Using palladium acetate as the catalyst, we arylated anilides, benzamides, benzoic acids, benzylamines, and 2-substituted pyridine derivatives under nearly identical conditions...
  16. ncbi Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor
    L L Thomsen
    Glaxo Wellcome Research and Development, Medicines Research Centre, Ware, Hertfordshire, United Kingdom
    Cancer Res 57:3300-4. 1997
    ..These studies confirm that nitric oxide production in tumors plays a role in promoting their growth, rather than a role as a host defense mechanism in inhibiting growth...
  17. pmc Calcium/calmodulin-dependent protein kinase II contributes to cardiac arrhythmogenesis in heart failure
    Can M Sag
    Department of Cardiology and Pneumology, Heart Center, Georg August University, Gottingen, Germany
    Circ Heart Fail 2:664-75. 2009
    ..We hypothesized that CaMKII contributes to arrhythmias and underlying cellular events and that inhibition of CaMKII reduces cardiac arrhythmogenesis in vitro and in vivo...
  18. pmc ATP-binding cassette transporter A1 mediates the beneficial effects of the liver X receptor agonist GW3965 on object recognition memory and amyloid burden in amyloid precursor protein/presenilin 1 mice
    James J Donkin
    Department of Pathology and Laboratory Medicine, Child and Family Research Institute, University of British Columbia, Vancouver, British Columbia V5Z 4H4, Canada
    J Biol Chem 285:34144-54. 2010
    ..These results suggest that ABCA1 contributes to several beneficial effects of the LXR agonist GW3965 in APP/PS1 mice...
  19. ncbi Raising HDL cholesterol without inducing hepatic steatosis and hypertriglyceridemia by a selective LXR modulator
    Bowman Miao
    Cardiovascular Biology, Bristol Myers Squibb Company, Experimental Station, Wilmington, DE 19880, USA
    J Lipid Res 45:1410-7. 2004
    ..This demonstration that tissue and gene selective modulation is possible with selective LXR modulators has positive implications for the development of this class of antiatherosclerotic agents...
  20. ncbi Liver X receptor agonists increase airway reactivity in a model of asthma via increasing airway smooth muscle growth
    Mark A Birrell
    Respiratory Pharmacology, Airway Disease Section, National Heart and Lung Institute, Faculty of Medicine, Imperial College London, London, United Kingdom
    J Immunol 181:4265-71. 2008
    ....
  21. ncbi Efficacy and tolerability of dapoxetine in treatment of premature ejaculation: an integrated analysis of two double-blind, randomised controlled trials
    Jon L Pryor
    University of Minnesota, Minneapolis, MN 55455, USA
    Lancet 368:929-37. 2006
    ..No drugs are approved for treatment of premature ejaculation. Our aim was to determine the efficacy and tolerability of on-demand dapoxetine in patients with severe premature ejaculation...
  22. pmc Ca2+/calmodulin-dependent protein kinase II alpha is required for the initiation and maintenance of opioid-induced hyperalgesia
    Yan Chen
    Department of Biopharmaceutical Sciences, University of Illinois, Chicago, Illinois 60612, USA
    J Neurosci 30:38-46. 2010
    ..These data implicate, for the first time, an essential role of CaMKIIalpha as a cellular mechanism leading to and maintaining opioid-induced hyperalgesia...
  23. ncbi Modulation of the hyperpolarization-activated current (I(f)) by calcium and calmodulin in the guinea-pig sino-atrial node
    Lauren Rigg
    Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK
    Cardiovasc Res 57:497-504. 2003
    ..Alterations in intracellular calcium during the cardiac cycle may be involved in fine tuning the voltage-dependent properties of I(f) and may thus determine its relative contribution to pacemaking in the SA node...
  24. ncbi Functional validation of Capsicum frutescens aminotransferase gene involved in vanillylamine biosynthesis using Agrobacterium mediated genetic transformation studies in Nicotiana tabacum and Capsicum frutescens calli cultures
    Harishchandra B Gururaj
    Plant Cell Biotechnology Department, Central Food Technological Research Institute, Constituent laboratory of Council of Scientific and Industrial Research, CSIR, Mysore 570020, India
    Plant Sci 195:96-105. 2012
    ..The result is a clear evidence of involvement of the reported putative aminotransferase responsible for vanillylamine biosynthesis in capsaicinoid biosynthesis pathway, confirming the gene function through functional validation...
  25. ncbi Calcium/calmodulin-dependent protein kinase II mediates cardioprotection of intermittent hypoxia against ischemic-reperfusion-induced cardiac dysfunction
    Zhuo Yu
    Key Laboratory of Stem Cell Biology, Institute of Health Sciences, Shanghai Jiao Tong University School of Medicine and Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Ruijin Hospital, Shanghai, China
    Am J Physiol Heart Circ Physiol 297:H735-42. 2009
    ..These findings indicate that preservation of SR CaMKII activity plays an important role in the IHA hypoxia-induced cardioprotection against I/R injury via maintaining SR Ca(2+)-uptake activity...
  26. ncbi Ximelagatran versus warfarin for stroke prevention in patients with nonvalvular atrial fibrillation. SPORTIF II: a dose-guiding, tolerability, and safety study
    Palle Petersen
    Department of Neurology, University State Hospital, Rigshospitalet, Copenhagen, Denmark
    J Am Coll Cardiol 41:1445-51. 2003
    ..We sought to compare the tolerability and safety of three fixed doses of ximelagatran versus warfarin in patients with nonvalvular atrial fibrillation (NVAF)...
  27. ncbi Semicarbazide-sensitive amine oxidase activity exerts insulin-like effects on glucose metabolism and insulin-signaling pathways in adipose cells
    Antonio Zorzano
    Facultat de Biologia, Departament de Bioquimica i Biologia Molecular, Universitat de Barcelona, Avda Diagonal 645, 08028 Barcelona, Spain
    Biochim Biophys Acta 1647:3-9. 2003
    ..Based on these observations, we propose that SSAO activity and vanadate potently mimic insulin effects in adipose cells and exert an anti-diabetic action in an animal model of type 1 diabetes mellitus...
  28. ncbi Functional loss of pAMT results in biosynthesis of capsinoids, capsaicinoid analogs, in Capsicum annuum cv. CH-19 Sweet
    Yaqin Lang
    Research Institute for Health Fundamentals, Ajinomoto Co Inc, 1 1 Suzuki cho, Kawasaki ku, Kawasaki 210 8681, Japan
    Plant J 59:953-61. 2009
    ..The dCAPS marker will be useful in selecting lines with capsinoid-containing fruits in pepper-breeding programs...
  29. ncbi Endotoxemia-mediated induction of cardiac inducible nitric-oxide synthase expression accounts for the hypotensive effect of ethanol in female rats
    Mahmoud M El-Mas
    Department of Pharmacology, School of Medicine, East Carolina University, Greenville, NC 27834, USA
    J Pharmacol Exp Ther 324:368-75. 2008
    ..These findings yield insight into the mechanistic role of endotoxin-myocardial iNOS signaling in the cardiodepressant action of ethanol, which accounts for its hypotensive effect in conscious female rats...
  30. ncbi A randomized, controlled, dose-guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I
    H Eriksson
    Department of Medicine, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    J Thromb Haemost 1:41-7. 2003
    ..Oral ximelagatran appears to be a promising alternative to current anticoagulant therapy to limit the progression of acute DVT, and it seems to possess a wide therapeutic window...
  31. pmc PP2B-dependent NO production in the medullary thick ascending limb during diabetes
    Jan M Foster
    Vascular Biology Center, Medical College of Georgia, Augusta, Georgia 30912, USA
    Am J Physiol Renal Physiol 297:F471-80. 2009
    ..In conclusion, while NO bioavailability in mTALs is reduced during diabetes, free radical scavenging with tempol unmasks increased NO production that involves PP2B-dependent activation of NOS1 and NOS2...
  32. pmc Acute inhibition of Ca2+/calmodulin-dependent protein kinase II reverses experimental neuropathic pain in mice
    Yan Chen
    Department of Biopharmaceutical Sciences, University of Illinois, Chicago, Illinois 60612, USA
    J Pharmacol Exp Ther 330:650-9. 2009
    ..In conclusion, our findings support a critical role of CaMKII in neuropathic pain. Blocking CaMKII or CaMKII-mediated signaling may offer a novel therapeutic target for the treatment of neuropathic pain...
  33. ncbi Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines
    Donald S Middleton
    Department of Discovery Chemistry B500, IPC 324, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 18:5303-6. 2008
    ..Overall, sulfonamide 20 was found to possess the best balance of target pharmacology, pharmacokinetics and metabolism profile...
  34. pmc Effects of DSP4 and methylphenidate on spatial memory performance in rats
    Thomas A Sontag
    Department of Experimental Psychology, University of Regensburg, 93040, Regensburg, Germany
    Atten Defic Hyperact Disord 3:351-8. 2011
    ..It is suggested that a reduction of noradrenaline and an increase of dopamine induce ADHD-related deficits and that the depletion of noradrenaline is not sufficient for an appropriate rat model of ADHD...
  35. ncbi DSP-4 prevents dopamine receptor priming by quinpirole
    Przemysław Nowak
    Department of Pharmacology, Medical University of Silesia, H Jordana 38 St, 41 808 Zabrze, Poland
    Pharmacol Biochem Behav 84:3-7. 2006
    ..The findings are supportive of a modulatory role of noradrenergic fibers on dopamine receptor priming (supersensitization) in rat brain...
  36. ncbi Costs and effectiveness of ximelagatran for stroke prophylaxis in chronic atrial fibrillation
    Cara L O'Brien
    Washington University School of Medicine, St Louis, MO 63110, USA
    JAMA 293:699-706. 2005
    ..Because ximelagatran can be taken in a fixed, oral dose without international normalized ratio monitoring and may have a lower risk of hemorrhage, it might improve quality-adjusted survival compared with dose-adjusted warfarin...
  37. ncbi PET measurement of serotonin transporter occupancy: a comparison of escitalopram and citalopram
    Johan Lundberg
    Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm, Sweden
    Int J Neuropsychopharmacol 10:777-85. 2007
    ..05). The small but significant difference in occupancy and K(i),(app) found between R,S-citalopram and S-citalopram suggests that not only S-citalopram but also R-citalopram to some degree occupies the 5-HTT in the human brain in vivo...
  38. ncbi Neonatal DSP-4 treatment modifies GABAergic neurotransmission in the prefrontal cortex of adult rats
    Aleksandra Bortel
    Department of Pharmacology, Medical University of Silesia, Jordana 38 St, 41 808 Zabrze, Poland
    Neurotox Res 13:247-52. 2008
    ..These findings indicate that neonatal DSP-4 treatment increases GABAergic neurotransmission in the PFC of rats in adulthood, perhaps by decreasing reactivity of central GABA(A) receptors...
  39. ncbi A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines
    Richard Apodaca
    Johnson and Johnson Pharmaceutical Research and Development, L L C, 3210 Merryfield Row, San Diego, California 92121, USA
    J Med Chem 46:3938-44. 2003
    4-(Aminoalkoxy)benzylamines were prepared and screened for in vitro activity at the human histamine H(3) receptor. Some members of this series exhibited subnanomolar binding affinities...
  40. ncbi Biomimetic oxidative coupling of benzylamines and 2-aminophenols: synthesis of benzoxazoles
    Yoshinori Endo
    Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, Sweden
    Chemistry 18:13609-13. 2012
    ..This biomimetic oxidation proceeds smoothly under mild conditions and the protocol can also be used for preparing benzimidazoles and benzothiazoles...
  41. ncbi Noradrenaline deficiency in brain increases beta-amyloid plaque burden in an animal model of Alzheimer's disease
    Sergey Kalinin
    Department of Anesthesiology, University of Illinois, and Jesse Brown Veteran s Affairs Research Division, Chicago, IL 60612, United States
    Neurobiol Aging 28:1206-14. 2007
    ..These findings suggest that noradrenergic innervation from LC are needed to maintain adequate Abeta clearance, and therefore that LC degeneration could contribute to AD pathogenesis...
  42. ncbi Desensitization of 5-HT(1A) autoreceptors induced by neonatal DSP-4 treatment
    Joanna Dabrowska
    Department of Pharmacology, Medical University of Silesia, 38 Jordana St, 41 808 Zabrze, Poland
    Eur Neuropsychopharmacol 17:129-37. 2007
    ..The nature of this phenomenon is attributable to the presynaptic adaptive mechanism and suggests the desensitization of 5-HT(1A) autoreceptors of rats with neonatal lesion of the central noradrenergic system...
  43. ncbi Quantification of 11C-MADAM binding to the serotonin transporter in the human brain
    Johan Lundberg
    Department of Clinical Neuroscience, Section of Psychiatry, Karolinska Institutet, Stockholm, Sweden
    J Nucl Med 46:1505-15. 2005
    ..The purpose of this study in humans was to examine the suitability and potential of (11)C-MADAM for quantitative PET studies of 5-HTT in applied clinical studies on the pathophysiology and treatment of neuropsychiatric disorders...
  44. ncbi KN-93 (2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated potassium channels
    Saman Rezazadeh
    Department of Cellular and Physiological Sciences, University of British Columbia, Vancouver, Canada
    J Pharmacol Exp Ther 317:292-9. 2006
    ..Importantly, KN-93 was ineffective as a blocker when applied intracellularly, suggesting that CaMK II-independent effects of KN-93 on Kv channels can be circumvented by intracellular application of KN-93...
  45. ncbi Measurement of serotonin transporter binding with PET and [11C]MADAM: a test-retest reproducibility study
    Johan Lundberg
    Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm, Sweden
    Synapse 60:256-63. 2006
    ..96 and 0.51 in the raphe nuclei and averaged bilateral regions. [(11)C]MADAM was shown to have good to excellent reliability in measurements of 5-HTT binding in brain regions of interest in research on psychiatric disorders...
  46. ncbi Neonatal N-(-2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4) treatment modifies the vulnerability to phenobarbital- and ethanol-evoked sedative-hypnotic effects in adult rats
    Aleksandra Bortel
    Department of Pharmacology, Medical University of Silesia, H Jordana 38, PL 41 808 Zabrze, Poland
    Pharmacol Rep 60:331-8. 2008
    ..These findings indicate that the noradrenergic system exerts a prominent influence on sedative-hypnotics acting via GABAergic systems in the brain without directly altering GABA levels in the brain...
  47. ncbi A PET study on regional coexpression of 5-HT1A receptors and 5-HTT in the human brain
    Johan Lundberg
    Department of Clinical Neuroscience, Section of Psychiatry, Karolinska Institutet, Stockholm, Sweden
    Psychopharmacology (Berl) 195:425-33. 2007
    ..Several lines of evidence suggest inter-dependency between the serotonin transporter (5-HTT) and the 5HT1A receptor, two recognised targets for the treatment of anxiety and depression...
  48. ncbi Role of coerulean noradrenergic neurones in general anaesthesia in rats
    T Kushikata
    Department of Anesthesiology, Hirosaki University Graduate School of Medicine, Hirosaki 036 8562, Japan
    Br J Anaesth 107:924-9. 2011
    ..We hypothesized that these neurones are also involved in both activation of the γ-aminobutyric acid type A (GABA(A)) receptor and inhibition of N-methyl-d-aspartate (NMDA) receptor-mediated anaesthesia...
  49. ncbi The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review
    David Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, S 431 83 Molndal, Sweden
    Thromb Res 109:S9-15. 2003
    ..As a consequence of its favourable pharmacokinetic and pharmacodynamic properties, ximelagatran is currently undergoing full-scale clinical development for the prophylaxis and treatment of thromboembolic disorders...
  50. pmc Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors
    Stanley F Barnett
    Department of Cancer Research, Merck and Company, Sumneytown Pike, West Point, PA 19454, USA
    Biochem J 385:399-408. 2005
    ....
  51. ncbi Beta-adrenergic enhancement of sarcoplasmic reticulum calcium leak in cardiac myocytes is mediated by calcium/calmodulin-dependent protein kinase
    Jerald Curran
    Rush University Medical Center, Chicago, IL 60611, USA
    Circ Res 100:391-8. 2007
    ..The results suggest that beta-AR stimulation enhances diastolic SR Ca leak in a manner that is (1) CaMKII dependent, (2) not protein kinase A dependent, and 3) not dependent on bulk [Ca](i)...
  52. ncbi The direct thrombin inhibitor melagatran followed by oral ximelagatran compared with enoxaparin for the prevention of venous thromboembolism after total hip or knee replacement: the EXPRESS study
    B I Eriksson
    Department of Orthopedics, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    J Thromb Haemost 1:2490-6. 2003
    ..Ximelagatran and its subcutaneous (s.c.) form melagatran are novel direct thrombin inhibitors for the prevention and treatment of thromboembolic disease...
  53. pmc Selective partial agonism of liver X receptor alpha is related to differential corepressor recruitment
    Caroline A Phelan
    Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, and The Institute for Diabetes, Obesity, and Metabolism, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Mol Endocrinol 22:2241-9. 2008
    ..Thus, differential recruitment of NCoR is a major determinant of partial agonism and selective LXR modulation of target genes...
  54. ncbi Synthetic LXR agonists increase LDL in CETP species
    Pieter H E Groot
    Cardiovascular Center for Excellence in Drug Discovery, GlaxoSmithKline, King of Prussia, Pa 19406 0939, USA
    J Lipid Res 46:2182-91. 2005
    ..These results reveal additional problems associated with current synthetic LXR agonists and emphasize the importance of profiling compounds in preclinical species with a more human-like LXR response and lipoprotein metabolism...
  55. ncbi Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement
    Charles W Francis
    Department of Medicine, University of Rochester, Rochester, NY, USA
    N Engl J Med 349:1703-12. 2003
    ..The purpose of the present study was to determine whether a higher dose of ximelagatran is superior to warfarin...
  56. ncbi Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects
    Ulf G Eriksson
    AstraZeneca R and D, 431 83 Mölndal, Sweden
    Eur J Clin Pharmacol 59:35-43. 2003
    ..The primary objectives were to determine the dose linearity and reproducibility of melagatran exposure and the influence of food intake...
  57. pmc Selective inhibition of iNOS attenuates trauma-hemorrhage/resuscitation-induced hepatic injury
    Wen Hong Kan
    Center for Surgical Research, University of Alabama at Birmingham, 1670 University Blvd, Birmingham, AL 35294 0019, USA
    J Appl Physiol (1985) 105:1076-82. 2008
    ..These results indicate that increased expression of iNOS following trauma-hemorrhage plays an important role in the induction of hepatic damage under such conditions...
  58. ncbi Effect of denervation of the locus coeruleus projections by DSP-4 treatment on [3H]-raclopride binding to dopamine D(2) receptors and D(2) receptor-G protein interaction in the rat striatum
    Jaanus Harro
    Department of Psychology, Center of Behavioral and Health Sciences, University of Tartu, EE 50410, Tartu, Estonia
    Brain Res 976:209-16. 2003
    ..Thus, alterations in the LC projection systems elicit lasting adaptive changes in DA-ergic neurotransmission that can serve as a substrate for psychiatric disorders...
  59. ncbi Dapoxetine for the treatment of premature ejaculation: results from a randomized, double-blind, placebo-controlled phase 3 trial in 22 countries
    Jacques Buvat
    CETPARP Le grand Hunier, Lille, France
    Eur Urol 55:957-67. 2009
    ..Dapoxetine is being developed for the on-demand treatment of premature ejaculation (PE). Previous clinical trials have demonstrated its safety and efficacy...
  60. ncbi [(11)C]MADAM, a new serotonin transporter radioligand characterized in the monkey brain by PET
    Christer Halldin
    Karolinska Institutet, Department of Clinical Neuroscience, Section of Psychiatry, Stockholm, Sweden
    Synapse 58:173-83. 2005
    ..The present characterization of binding in the monkey brain suggests that [(11)C]MADAM is a potential PET radioligand for quantitative studies of 5-HTT binding in the human brain...
  61. ncbi Pharmacokinetics of dapoxetine hydrochloride in healthy Chinese, Japanese, and Caucasian men
    An Thyssen
    Johnson and Johnson Pharmaceutical Research and Development, Division of Janssen Pharmaceutica, NV, Turnhoutseweg 30 B 2340 Beerse, Belgium
    J Clin Pharmacol 50:1450-60. 2010
    ..Dapoxetine was well tolerated by all 3 ethnic groups...
  62. ncbi Mechanism of action of the oral direct thrombin inhibitor ximelagatran
    Christer Mattsson
    AstraZeneca, Molndal, Sweden
    Semin Vasc Med 5:235-44. 2005
    ..The combination of antithrombotic and anti-inflammatory activity with the practicality of oral dosing provided by ximelagatran represents an important new option for the treatment of arterial and venous thromboembolic disorders...
  63. ncbi Effect of melagatran on prothrombin time assays depends on the sensitivity of the thromboplastin and the final dilution of the plasma sample
    C Mattsson
    Department of Cell Biology and Biochemistry, AstraZeneca R and D, Molndal, Sweden
    Thromb Haemost 86:611-5. 2001
    ..Thus, since the same melagatran concentration can be associated with widely varying PT/INR results depending on the specific assay used it is concluded that PT assays and INR can not be used to monitor melagatran activity...
  64. ncbi Pharmacokinetics of dapoxetine, a new treatment for premature ejaculation: Impact of age and effects of a high-fat meal
    Mark J Dresser
    ALZA Corporation, 1900 Charleston Road, Building M11 4, Mountain View, CA 94043, USA
    J Clin Pharmacol 46:1023-9. 2006
    ..Thus, age or consumption of a high-fat meal has only a modest impact on dapoxetine pharmacokinetics in healthy men...
  65. ncbi Treatment of premature ejaculation in the Asia-Pacific region: results from a phase III double-blind, parallel-group study of dapoxetine
    Chris McMahon
    Australian Centre for Sexual Health, University of Sydney, NSW, Australia
    J Sex Med 7:256-68. 2010
    ..Dapoxetine is a short-acting selective serotonin reuptake inhibitor that was recently approved for the on-demand treatment of premature ejaculation (PE)...
  66. ncbi Thrombin-induced platelet activation and its inhibition by anticoagulants with different modes of action
    Sven Nylander
    Cell Biology and Biochemistry, Preclinical R and D, AstraZeneca R and D Molndal, Sweden
    Blood Coagul Fibrinolysis 14:159-67. 2003
    ..Thus, reversible direct thrombin inhibitors, such as melagatran, are potent inhibitors of thrombin-induced platelet activation, acting mainly by inhibition of a PAR-1-independent component...
  67. ncbi Dapoxetine for premature ejaculation
    Chris G McMahon
    Australian Centre for Sexual Health, Suite 2 4, Berry Road Medical Centre, 1a Berry Road, St Leonards, NSW 2065, Australia
    Expert Opin Pharmacother 11:1741-52. 2010
    ..Drug treatment of PE with an off-label antidepressant selective serotonin reuptake inhibitor (SSRI) drug is common. The lack of an approved drug and total reliance on off-label treatment represents a substantial unmet treatment need...
  68. ncbi Predicting the pharmacology of thrombin inhibitors
    T E Adams
    Department of Biochemistry, University of Vermont, College of Medicine, Burlington, Vermont 05405, USA
    J Thromb Haemost 1:1024-7. 2003
    ..The data suggest that numerical models will be useful in predicting the effectiveness of inhibitors of coagulation...
  69. ncbi Ximelagatran compared with warfarin for prevention of thromboembolism in patients with nonvalvular atrial fibrillation: Rationale, objectives, and design of a pair of clinical studies and baseline patient characteristics (SPORTIF III and V)
    Jonathan L Halperin
    Zena and Michael A Wiener Cardiovascular Institute, Mount Sinai Medical Center, New York, NY 10029 6574, USA
    Am Heart J 146:431-8. 2003
    ..0-3.0)...
  70. ncbi Treatment benefit of dapoxetine for premature ejaculation: results from a placebo-controlled phase III trial
    Joel M Kaufman
    Urology Research Options, Aurora, CO 80012, USA
    BJU Int 103:651-8. 2009
    ..Although these factors are key elements of numerous sets of diagnostic criteria for PE, they have rarely been evaluated as outcome measures in clinical trials...
  71. ncbi Pharmacokinetic, pharmacodynamic, and electrocardiographic effects of dapoxetine and moxifloxacin compared with placebo in healthy adult male subjects
    Nishit B Modi
    Johnson and Johnson Pharmaceutical Research and Development, 700 US Route 202, Raritan, NJ 08869, USA
    J Clin Pharmacol 49:634-42. 2009
    ..Adverse events are generally mild in severity; nausea is the most common. The results demonstrate that dapoxetine does not have electrocardiographic effects at doses of 60, 120, and 240 mg...
  72. ncbi Pharmacokinetics of ximelagatran and relationship to clinical response in acute deep vein thrombosis
    Marie Cullberg
    Clinical Pharmacology and Clinical Cardiovascular, AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacol Ther 77:279-90. 2005
    ....
  73. ncbi Single- and multiple-dose pharmacokinetics of dapoxetine hydrochloride, a novel agent for the treatment of premature ejaculation
    Nishit B Modi
    ALZA Corporation, 1900 Charleston Road, Building M11 4A, Mountain View, CA 94043, USA
    J Clin Pharmacol 46:301-9. 2006
    ..There were no serious adverse events; the most commonly reported adverse events were diarrhea, dizziness, and nausea...
  74. ncbi Quinpramine--a promising compound for treating immune-mediated demyelination of the nervous system
    Gerd Meyer zu Horste
    Department of Neurology, Heinrich Heine University, Dusseldorf, Germany
    Drug News Perspect 23:287-94. 2010
    ..This article summarizes available treatment options in MS and explains why the candidate compound quinpramine may transfer from bench to bedside in the near future...
  75. ncbi Effects of the noradrenergic neurotoxin DSP4 on spatial memory in the rat
    T A Sontag
    Department of Experimental Psychology, University of Regensburg, Regensburg, Germany
    J Neural Transm 115:299-303. 2008
    ..The use of different doses of DSP4 to influence prefrontal functions and to understand the dysbalance of dopamine and noradrenaline in ADHD appears to be a promising approach...
  76. ncbi CaMKII-independent effects of KN93 and its inactive analog KN92: reversible inhibition of L-type calcium channels
    Lei Gao
    Department of Molecular Pharmacology, Physiology and Biotechnology, Brown University, Providence, RI 02912, USA
    Biochem Biophys Res Commun 345:1606-10. 2006
    ..Together, our data suggest that, in addition to inhibiting CaMKII, KN93 also affects CaV1.3 and CaV1.2 calcium channels in a CaMKII-independent manner...
  77. ncbi Perceived control over ejaculation is central to treatment benefit in men with premature ejaculation: results from phase III trials with dapoxetine
    Ridwan Shabsigh
    Division of Urology, Maimonides Medical Center, Columbia University, New York, NY 11219, USA
    BJU Int 102:824-8. 2008
    ....
  78. pmc Increased intracellular Ca2+ and SR Ca2+ load contribute to arrhythmias after acidosis in rat heart. Role of Ca2+/calmodulin-dependent protein kinase II
    M Said
    Centro de Investigaciones Cardiovasculares, Facultad de Ciencias Medicas, Universidad Nacional de La Plata, La Plata, Argentina
    Am J Physiol Heart Circ Physiol 295:H1669-83. 2008
    ..The results reveal that arrhythmias after acidosis are dependent on CaMKII activation and are associated with an increase in SR Ca(2+) load, which appears to be mainly due to the increase in PT-PLN...
  79. ncbi The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects
    D Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D Molndal, S 431 83, Molndal, Sweden
    Thromb Res 101:171-81. 2001
    ..In an experimental thrombosis model in the rat, oral H 376/95 was more effective than the subcutaneous low molecular weight heparin dalteparin in preventing thrombosis...
  80. ncbi Phospholipase C-gamma, protein kinase C and Ca2+/calmodulin-dependent protein kinase II are involved in platelet-derived growth factor-induced phosphorylation of Tiam1
    I N Fleming
    Howard Hughes Medical Institute and Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    FEBS Lett 429:229-33. 1998
    ..Moreover, PDGF-stimulated Tiam1 phosphorylation was markedly reduced by 72 +/- 10% in PLC-gamma1 deficient mouse fibroblasts, compared to wild-type cells, indicating that phosphoinositide phospholipase C is involved...
  81. ncbi A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibition in
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    Thromb Haemost 87:231-7. 2002
    ..Ximelagatran and melagatran were well tolerated. In conclusion, ximelagatran and its active form melagatran appear to be promising agents for the prevention of venous thromboembolism following orthopaedic surgery...
  82. ncbi Calmodulin kinase II and arrhythmias in a mouse model of cardiac hypertrophy
    Yuejin Wu
    Department of Internal Medicine, Vanderbilt University, Nashville, Tenn, USA
    Circulation 106:1288-93. 2002
    ..CaMKII upregulation and prolonged repolarization are general features of cardiomyopathy, but the role of CaMKII in arrhythmias in cardiomyopathy is unknown...
  83. ncbi Ximelagatran vs warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a randomized trial
    Gregory W Albers
    Stanford Stroke Center, Palo Alto, Calif, USA
    JAMA 293:690-8. 2005
    ..In patients with nonvalvular atrial fibrillation, warfarin prevents ischemic stroke, but dose adjustment, coagulation monitoring, and bleeding limit its use...
  84. ncbi CaMKII inhibition protects against necrosis and apoptosis in irreversible ischemia-reperfusion injury
    Martin Vila-Petroff
    Centro de Investigaciones Cardiovasculares, Facultad de Ciencias Medicas, 60 y 120, 1900 La Plata, Argentina
    Cardiovasc Res 73:689-98. 2007
    ..The goal of the present study is to investigate the role of CaMKII in irreversible ischemia and reperfusion (I/R) injury...
  85. ncbi Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    Lancet 360:1441-7. 2002
    ..We aimed to compare the efficacy and safety with that of dalteparin...
  86. ncbi Noradrenergic depletion potentiates beta -amyloid-induced cortical inflammation: implications for Alzheimer's disease
    Michael T Heneka
    Department of Neurology, University of Bonn, Germany 53127
    J Neurosci 22:2434-42. 2002
    ..These data demonstrate that LC loss and NE depletion augment inflammatory responses to Abeta and suggest that LC loss in AD is permissive for increased inflammation and neuronal cell death...
  87. ncbi Direct thrombin inhibitor melagatran followed by oral ximelagatran in comparison with enoxaparin for prevention of venous thromboembolism after total hip or knee replacement
    Bengt I Eriksson
    Orthopaedics Department, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    Thromb Haemost 89:288-96. 2003
    ..0%) and 306/1122 (27.3%) patients in the ximelagatran and enoxaparin group, respectively, a difference in risk of 3.7% in favour of enoxaparin (p = 0.053). Bleeding was comparable between the two groups...
  88. ncbi Activation of liver X receptors promotes neuroprotection and reduces brain inflammation in experimental stroke
    Jesús R Morales
    Department of Pharmacology, School of Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain
    Circulation 118:1450-9. 2008
    ..These beneficial actions, however, have not been illustrated in other models of acute injury such as stroke in which inflammation is an important pathophysiological feature...
  89. ncbi Comparison of ximelagatran, an oral direct thrombin inhibitor, with enoxaparin for the prevention of venous thromboembolism following total hip replacement. A randomized, double-blind study
    C W Colwell
    Scripps Clinic Center for Orthopaedic Research and Education, 11025 North Torrey Pines Road, Suite 140, La Jolla, CA 92037 1030, USA
    J Thromb Haemost 1:2119-30. 2003
    ..We compared the efficacy and safety of ximelagatran with those of enoxaparin for the prevention of VTE in patients undergoing THR...
  90. pmc Treatment with LXR agonists after focal cerebral ischemia prevents brain damage
    Luigi Sironi
    Department of Pharmacological Sciences, University of Milan, via G Balzaretti 9, 20133 Milan, Italy
    FEBS Lett 582:3396-400. 2008
    ..Neuroprotection was associated with suppression of neuroinflammation...
  91. ncbi Phospholamban is required for CaMKII-dependent recovery of Ca transients and SR Ca reuptake during acidosis in cardiac myocytes
    J DeSantiago
    Department of Physiology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL 60153, USA
    J Mol Cell Cardiol 36:67-74. 2004
    ..We conclude that PLB is crucial to the recovery of Delta[Ca]i and k(Ca) during acidosis. Moreover, PLB phosphorylation by CaMKII plays an important role in limiting the decline in Ca transients (and contraction) during acidosis...
  92. ncbi Noradrenergic depletion increases inflammatory responses in brain: effects on IkappaB and HSP70 expression
    Michael T Heneka
    Department of Neurology, University of Bonn, Germany
    J Neurochem 85:387-98. 2003
    ..These findings suggest one mechanism by which PPARgamma agonists could provide benefit in neurological diseases having an inflammatory component...
  93. ncbi The benefit-to-risk profile of melagatran is superior to that of hirudin in a rabbit arterial thrombosis prevention and bleeding model
    P Klement
    McMaster University and Henderson Research Center, Hamilton, Ontario, Canada
    J Thromb Haemost 1:587-94. 2003
    ..Thus, at maximally effective doses, melagatran causes less bleeding than hirudin in this model. These findings raise the possibility that some direct thrombin inhibitors are safer than others...
  94. ncbi Ximelagatran versus warfarin for the prevention of venous thromboembolism after total knee arthroplasty. A randomized, double-blind trial
    Charles W Francis
    University of Rochester School of Medicine and Dentistry, Rochester, New York, USA
    Ann Intern Med 137:648-55. 2002
    ..Ximelagatran, an oral direct thrombin inhibitor, has shown promising efficacy and tolerability in patients undergoing total hip or knee arthroplasty...
  95. ncbi Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement: a phase 2 dose-finding study
    J A Heit
    Division of Cardiovascular Diseases, Hematology Research, Mayo Clinic, 200 First St SW, Rochester, MN 55905
    Arch Intern Med 161:2215-21. 2001
    ..CONCLUSION: Fixed-dose, unmonitored ximelagatran, 24 mg twice daily, given after surgery appears to be safe and effective oral prophylaxis against venous thromboembolism after total knee replacement...
  96. ncbi Effects of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, and dalteparin on the endogenous thrombin potential in venous blood from healthy male subjects
    Stig L Boström
    AstraZeneca R and D, Molndal, Sweden
    Blood Coagul Fibrinolysis 14:457-62. 2003
    ..Thus, melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, efficiently delays and inhibits the generation of thrombin in plasma both in vitro and ex vivo...
  97. ncbi Pharmacokinetics of melagatran and the effect on ex vivo coagulation time in orthopaedic surgery patients receiving subcutaneous melagatran and oral ximelagatran: a population model analysis
    Ulf G Eriksson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacokinet 42:687-701. 2003
    ..To support the design of a pivotal dose-finding study, the impact of individualised dosage based on bodyweight and calculated creatinine clearance was examined...
  98. ncbi Pharmacokinetics and anticoagulant effect of the direct thrombin inhibitor melagatran following subcutaneous administration to healthy young men
    Susanne Johansson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Blood Coagul Fibrinolysis 14:677-84. 2003
    ..Only moderate increases in capillary bleeding time were observed with s.c. doses up to 5 mg melagatran. Melagatran was well tolerated after s.c. injection, with good local tolerability at the injection site...
  99. ncbi Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran
    Ulf G Eriksson
    Experimental Medicine, AstraZeneca R and D, Molndal, Sweden
    Clin Pharmacokinet 42:743-53. 2003
    ..After oral administration, ximelagatran is rapidly absorbed and bioconverted to its active form, melagatran...
  100. ncbi Inhibition of thrombin-induced feedback activation of factor V: a potential pathway for inhibition of thrombin generation by melagatran
    Stig L Boström
    AstraZeneca R and D, Molndal, Sweden
    Blood Coagul Fibrinolysis 15:25-30. 2004
    ..These results indicate that inhibition of thrombin-mediated amplification reactions in blood coagulation is an effective way to delay or inhibit thrombin generation...
  101. ncbi The beginning of the end of warfarin?
    John W Eikelboom
    Med J Aust 180:549-51. 2004

Research Grants45

  1. Alcohol Modulation of Cerebellar Synaptic Currents
    William Proctor; Fiscal Year: 2006
    ..The combination of our proposed and ongoing genetic studies may aid the identification of more sensitive drug targets and the development of novel drugs for rational therapeutic approaches to alcoholism. ..
  2. Characterization of Sleep Mutants of Drososphila
    Chiara Cirelli; Fiscal Year: 2009
    ..This research will help to identify the molecular mechanisms regulating the need for sleep and provide novel clues to its functions. ..
  3. Inflammation and Infection as Risk Factors in Stroke
    Mitchell Elkind; Fiscal Year: 2006
    ..Nationally recognized experts in stroke epidemiology and basic vascular biology will serve as mentors for these studies. ..
  4. Novel anesthetic mechanisms that desensitize nociceptors
    Lieju Liu; Fiscal Year: 2006
    ..This information will lead to novel anesthetic mechanisms that involve the reversible desensitization of nociceptors. ..
  5. Imaging vesicular monoamine transporters in the brain
    HANK KUNG; Fiscal Year: 2006
    ..Michael Kilbourn, University of Michigan. Combining the strength of two laboratories will greatly enhance the chance of reaching the goals proposed in this project. ..
  6. PET Imaging MDMA Neurotoxicity
    Una McCann; Fiscal Year: 2006
    ..g., dementia, Parkinsonism, depression/anxiety). In addition, the proposed 18FDG studies will address the question of if MDMA exposure leads to altered brain function at the most fundamental level, glucose utilization. ..
  7. SAFER THROMBOLYTIC THERAPY USING PLASMIN
    Victor Marder; Fiscal Year: 2007
    ..We hypothesize and anticipate that plasmin will provide clinically effective thrombolysis without an increased risk of bleeding . ..
  8. New imaging agents for studying gene expression
    HANK KUNG; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  9. CNS mechanisms of black cohosh in menopause
    Zaijie Jim Wang; Fiscal Year: 2007
    ..Data gained from these studies will provide a foundation that will ultimately lead to novel approaches for preventing and controlling menopausal symptoms. ..
  10. Sex Differences in Brain and Behavior Development
    Juli Wade; Fiscal Year: 2007
    ....
  11. Inflammatory and Infectious Burden and Risk of Stroke
    Mitchell Elkind; Fiscal Year: 2008
    ..The cross-sectional associations between inflammatory and infectious markers and quantitative MRI abnormalities will also be assessed. ..
  12. Nanoparticle targeting of cathepsin-L inhibitor and doxorubicin in breast cancer
    Shaker Mousa; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  13. Neuropharmacology of GHB discrimination
    Wouter Koek; Fiscal Year: 2010
    ..Increased knowledge about the activation and modulation of GABAB systems will help to develop effective approaches to treating sleep-, drug abuse-, and other CNS disorders. ..
  14. Levels of Inflammatory Markers in Treatment of Stroke
    Mitchell Elkind; Fiscal Year: 2008
    ..abstract_text> ..
  15. Biological Predictors of Response to Antidepressants
    Ramin V Parsey; Fiscal Year: 2010
    ..Our overall goal is to reduce the trial and error associated with finding an effective antidepressant by using data from pre-treatment quantification of 5-HT1A receptors and 5-HTT to guide antidepressant treatment selection. ..
  16. Molecular mechanisms of Vitex agnus-castus L. in PMS
    Zaijie Jim Wang; Fiscal Year: 2005
    ..Data from the current study will help to improve or develop novel therapies for the treatment of PMS. ..
  17. NEW TC-99M LABELED BRAIN IMAGING AGENTS
    HANK KUNG; Fiscal Year: 2004
    ..If the novel DAT imaging agents are successfully developed, the new Tc-99m labeled imaging agents will be scientifically meaningful and clinically important for the diagnosis of Parkinson's disease. ..
  18. NEW TC-99M LABELED BRAIN IMAGING AGENTS
    HANK KUNG; Fiscal Year: 2001
    ..If the novel DAT imaging agents are successfully developed, the new Tc-99m labeled imaging agents will be scientifically meaningful and clinically important for the diagnosis of Parkinson's disease. ..
  19. Molecular Mechanisms of Receptor Function in SE
    SEVERN CHURN; Fiscal Year: 2005
    ..Understanding the cellular mechanisms that result in altered GABAAR function in SE is essential to the development of new treatment strategies to manage SE in the clinical setting. ..
  20. SEROTONIN RECEPTOR LIGANDS FOR SPECT IMAGING
    HANK KUNG; Fiscal Year: 2001
    ..The novel imaging agents may lead to simple and useful routine diagnostic procedures for various mental health diseases involving SERT in the brain. ..
  21. A MULTI-CENTER THERAPY TRIAL FOR ACUTE LIVER FAILURE
    William Lee; Fiscal Year: 2004
    ..The overall goal is to apply modern clinical, epidemiological and virological techniques to the study of this rare but devastating illness. ..
  22. DYNORPHIN MODULATES CGRP RELEASE VIA PKC
    Zaijie Jim Wang; Fiscal Year: 2003
    ..Frank Porreca and Josephine Lai. This award is consistent with the long-term career goal of the candidate to become an independent investigator contributing to the basic research of pain and opioid pharmacology. ..
  23. MECHANISMS OF ANESTHETIC ACTION ON SMOOTH MUSCLE
    JUDY SU; Fiscal Year: 2004
    ..Further the understanding of signal pathways of CaMKII and PKC in smooth muscle will advance understanding mechanisms of agonist-activated force maintenance in smooth muscle, as well as cell motility and migration in non-muscle cells. ..
  24. NEW CNS DOPAMINE RECEPTOR IMAGING AGENTS
    HANK KUNG; Fiscal Year: 2002
    ....
  25. In vivo imaging agents targeting Tau aggregates
    HANK KUNG; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  26. DOPAMINE TRANSPORTER IMAGING WITH FLUORINE-18 PET
    JOHN NEUMEYER; Fiscal Year: 2003
    ..The lead compound in this series (presently BRL-308) will be evaluated by PET imaging and pharmacokinetics, in non-human primates. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE ..
  27. Mechanisms Underlying the Cognitive Function of Sleep
    Subimal Datta; Fiscal Year: 2009
    ....
  28. SEROTONIN RECEPTOR LIGANDS FOR SPECT IMAGING
    HANK KUNG; Fiscal Year: 2004
    ..The novel imaging agents may lead to simple and useful routine diagnostic procedures for various mental health diseases involving SERT in the brain. ..
  29. AUTOMATED CARDIAC DECISION SUPPORT SYSTEM IMPROVES CARE
    Lawrence Baruch; Fiscal Year: 2005
    ..If this automated clinical information and decision support system is successful and widely implemented, the best outcomes from care for chronic cardiovascular disease may be achieved. ..
  30. Quality of Life of Overweight Youth: Multicultural View
    Donald Patrick; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  31. Imaging of Serotonin Transporters in Depression
    RAMIN PARSEY; Fiscal Year: 2005
    ..These goals will be met by a combination of didactic I course work and supervision. ..
  32. Imaging agents of norepinephrine transporters
    HANK KUNG; Fiscal Year: 2007
    ..abstract_text> ..
  33. Role of Pancreatic Trypsin Inhibitors in Pancreatic
    Rodger A Liddle; Fiscal Year: 2010
    ..abstract_text> ..
  34. BRAIN SEROTONIN TRANSPORTER IN ECSTASY AND MDA USERS
    Stephen Kish; Fiscal Year: 2007
    ..More broadly, our data will help define the contribution of different neuroanatomical components of the brain serotonin system to human behavior. ..
  35. Sleep and Nocturnal Endocrine Function in MDMA User
    Una McCann; Fiscal Year: 2007
    ..Results from the proposed studies will help better define the functional consequences of MDMA exposure in humans, and could shed light on the roles of 5-HT and DA in sleep and nocturnal endocrine function. ..
  36. Software Promotes NCEP/AHA Provider Guideline Adherence
    Lawrence Baruch; Fiscal Year: 2003
    ..If this automated clinical information and decision support system is successful and widely implemented, the best outcomes from care for chronic cardiovascular disease may be achieved. ..
  37. 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. ..
  38. Discriminative Stimulus Effects of Alcohol in Mice
    Wouter Koek; Fiscal Year: 2007
    ..This future research will increase our understanding of risk factors for alcoholism and drug abuse and will help the development of effective approaches to prevention and treatment. [unreadable] [unreadable] [unreadable]..
  39. Role of calcium-dependent mechanisms in nicotine's tolerance and effects
    MOHAMAD IMAD DAMAJ; Fiscal Year: 2010
    ..The proposed studies will help elucidate the molecular basis of nicotine dependence as well as the Ca2+ dependent neuroadaptation processes that occurs after short-and long-term exposure to this drug of abuse. ..
  40. Hearing Loss and Quality of Life of Children and Youth
    Donald Patrick; Fiscal Year: 2009
    ....
  41. Role of Lamin B Receptor in Neutrophil Maturation and Functional Activation
    Peter Gaines; Fiscal Year: 2007
    ..The results may also offer important insight into the pathogenesis of potentially fatal hematologic disorders. [unreadable] [unreadable] [unreadable]..
  42. 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. ..
  43. NEUROENDOCRINE CONTROL OF REPRODUCTIVE BEHAVIOR
    LAUREN RITERS; Fiscal Year: 2003
    ..In addition, this research could lay the groundwork for future studies on the etiology of disorders related to sexual arousal...
  44. SOFTWARE EFFECT ON PROMOTING ADHERENCE TO CHF GUIDELINES
    Lawrence Baruch; Fiscal Year: 2005
    ..If this decision support system is successful and widely implemented, the best outcomes from care for chronic heart failure may be achieved. ..
  45. Viral-Mediated Alterations in CaMKII Alter Behavioral Responding to Amphetamine
    Jessica Loweth; Fiscal Year: 2008
    ..This research will contribute to the ultimate goal of preventing drug addiction by investigating ways to prevent the enhanced drug taking observed in rats that have been previously exposed to AMPH. [unreadable] [unreadable] [unreadable]..