guanidines

Summary

Summary: A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.

Top Publications

  1. pmc Mutations in a conserved residue in the influenza virus neuraminidase active site decreases sensitivity to Neu5Ac2en-derived inhibitors
    J L McKimm-Breschkin
    Biomolecular Research Institute, Parkville, Australia
    J Virol 72:2456-62. 1998
  2. pmc AMP kinase is required for mitochondrial biogenesis in skeletal muscle in response to chronic energy deprivation
    Haihong Zong
    Howard Hughes Medical Institute and the Departments of Internal Medicine, Cell Biology, and Cellular and Molecular Physiology, Yale University School of Medicine, New Haven, CT 06510, USA
    Proc Natl Acad Sci U S A 99:15983-7. 2002
  3. pmc Hoe 694, a new Na+/H+ exchange inhibitor and its effects in cardiac ischaemia
    W Scholz
    Hoechst AG, Frankfurt M, Germany
    Br J Pharmacol 109:562-8. 1993
  4. ncbi Neonicotinoid insecticides display partial and super agonist actions on native insect nicotinic acetylcholine receptors
    Laurence A Brown
    Department of Physiology, Anatomy and Genetics, MRC Functional Genetics Unit, Le Gros Clark Building, University of Oxford, South Parks Road, Oxford, UK
    J Neurochem 99:608-15. 2006
  5. ncbi Efficacy of dinotefuran-pyriproxyfen, dinotefuran-pyriproxyfen-permethrin and fipronil-(S)-methoprene topical spot-on formulations to control flea populations in naturally infested pets and private residences in Tampa, FL
    Michael W Dryden
    Dept of Diagnostic Medicine Pathobiology, Kansas State University, Manhattan, KS, USA
    Vet Parasitol 182:281-6. 2011
  6. pmc Nalfurafine prevents 5'-guanidinonaltrindole- and compound 48/80-induced spinal c-fos expression and attenuates 5'-guanidinonaltrindole-elicited scratching behavior in mice
    S Inan
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    Neuroscience 163:23-33. 2009
  7. ncbi Use of aminoguanidine (Pimagedine) to prevent the formation of advanced glycation endproducts
    Paul J Thornalley
    Department of Biological Sciences, University of Essex, Central Campus, Wivenhoe Park, Colchester, CO4 3SQ, Essex, UK
    Arch Biochem Biophys 419:31-40. 2003
  8. ncbi The creatine transporter mediates the uptake of creatine by brain tissue, but not the uptake of two creatine-derived compounds
    G Lunardi
    Section of Pharmacology, Department of Oncology, Biology and Genetics, University of Genova, Genova, Italy
    Neuroscience 142:991-7. 2006
  9. pmc The complement inhibitor FUT-175 suppresses T cell autoreactivity in experimental autoimmune encephalomyelitis
    Qing Li
    Assistant Professor, Institute of Pathology, Case Western Reserve University School of Medicine, 2085 Adelbert Road, Room 306, Cleveland, OH 44106, USA
    Am J Pathol 175:661-7. 2009
  10. ncbi Prevention of diabetic vascular dysfunction by guanidines. Inhibition of nitric oxide synthase versus advanced glycation end-product formation
    R G Tilton
    Department of Ophthalmology, Washington University School of Medicine, St Louis, MO 63110
    Diabetes 42:221-32. 1993

Detail Information

Publications269 found, 100 shown here

  1. pmc Mutations in a conserved residue in the influenza virus neuraminidase active site decreases sensitivity to Neu5Ac2en-derived inhibitors
    J L McKimm-Breschkin
    Biomolecular Research Institute, Parkville, Australia
    J Virol 72:2456-62. 1998
    ..Altered binding of the hydrophobic side chain at the 6 position or the triol group could account for the decreased binding of both the NA inhibitors and substrate...
  2. pmc AMP kinase is required for mitochondrial biogenesis in skeletal muscle in response to chronic energy deprivation
    Haihong Zong
    Howard Hughes Medical Institute and the Departments of Internal Medicine, Cell Biology, and Cellular and Molecular Physiology, Yale University School of Medicine, New Haven, CT 06510, USA
    Proc Natl Acad Sci U S A 99:15983-7. 2002
    ..These data demonstrate that by sensing the energy status of the muscle cell, AMPK is a critical regulator involved in initiating mitochondrial biogenesis...
  3. pmc Hoe 694, a new Na+/H+ exchange inhibitor and its effects in cardiac ischaemia
    W Scholz
    Hoechst AG, Frankfurt M, Germany
    Br J Pharmacol 109:562-8. 1993
    ..In view of the role which Na+/H+ exchange seems to play in the pathophysiology of cardiac ischaemia these effects could probably be attributed to Na+/H+ exchange inhibition...
  4. ncbi Neonicotinoid insecticides display partial and super agonist actions on native insect nicotinic acetylcholine receptors
    Laurence A Brown
    Department of Physiology, Anatomy and Genetics, MRC Functional Genetics Unit, Le Gros Clark Building, University of Oxford, South Parks Road, Oxford, UK
    J Neurochem 99:608-15. 2006
    ..Cell-attached recordings indicate that super agonism results from more frequent openings at the largest (63.5 pS) conductance state observed...
  5. ncbi Efficacy of dinotefuran-pyriproxyfen, dinotefuran-pyriproxyfen-permethrin and fipronil-(S)-methoprene topical spot-on formulations to control flea populations in naturally infested pets and private residences in Tampa, FL
    Michael W Dryden
    Dept of Diagnostic Medicine Pathobiology, Kansas State University, Manhattan, KS, USA
    Vet Parasitol 182:281-6. 2011
    ..24% and 95.47%, respectively. Flea numbers in the indoor-premises were also markedly reduced by days 54-60, with 98.05% and 96.15% reductions in intermittent-light flea trap counts in the DP-DPP or FM treatment groups, respectively...
  6. pmc Nalfurafine prevents 5'-guanidinonaltrindole- and compound 48/80-induced spinal c-fos expression and attenuates 5'-guanidinonaltrindole-elicited scratching behavior in mice
    S Inan
    Department of Pharmacology, Temple University School of Medicine, 3420 North Broad Street, Philadelphia, PA 19140, USA
    Neuroscience 163:23-33. 2009
    ..On the basis of our results, nalfurafine holds promise as a potentially useful antipruritic in human conditions involving itch...
  7. ncbi Use of aminoguanidine (Pimagedine) to prevent the formation of advanced glycation endproducts
    Paul J Thornalley
    Department of Biological Sciences, University of Essex, Central Campus, Wivenhoe Park, Colchester, CO4 3SQ, Essex, UK
    Arch Biochem Biophys 419:31-40. 2003
    ..Pharmacological scavenging of alpha-oxoaldehydes or stimulation of host alpha-oxoaldehyde detoxification remains a worthy therapeutic strategy to prevent diabetic complications and other AGE-related disorders...
  8. ncbi The creatine transporter mediates the uptake of creatine by brain tissue, but not the uptake of two creatine-derived compounds
    G Lunardi
    Section of Pharmacology, Department of Oncology, Biology and Genetics, University of Genova, Genova, Italy
    Neuroscience 142:991-7. 2006
    ..CrOBzl and PCr-Mg-CPLX cross the plasma membrane in a transporter-independent way, and might be useful in the therapy of hereditary creatine transporter deficiency. They may also prove useful in the therapy of brain anoxia or ischemia...
  9. pmc The complement inhibitor FUT-175 suppresses T cell autoreactivity in experimental autoimmune encephalomyelitis
    Qing Li
    Assistant Professor, Institute of Pathology, Case Western Reserve University School of Medicine, 2085 Adelbert Road, Room 306, Cleveland, OH 44106, USA
    Am J Pathol 175:661-7. 2009
    ..These results argue that complement regulators, which inhibit C5a/C3a production, may have therapeutic efficacy in multiple sclerosis and in other clinical conditions in which T cells drive disease pathogenesis...
  10. ncbi Prevention of diabetic vascular dysfunction by guanidines. Inhibition of nitric oxide synthase versus advanced glycation end-product formation
    R G Tilton
    Department of Ophthalmology, Washington University School of Medicine, St Louis, MO 63110
    Diabetes 42:221-32. 1993
    ....
  11. pmc Rapid selection of oseltamivir- and peramivir-resistant pandemic H1N1 virus during therapy in 2 immunocompromised hosts
    Matthew J Memoli
    Viral Pathogenesis and Evolution Section, Laboratory of Infectious Diseases, National Institutes of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892 3203, USA
    Clin Infect Dis 50:1252-5. 2010
    ..We describe rapid selection for the H275Y resistance mutation during therapy in 2 immunocompromised individuals at 9 and 14 days of therapy, as well as the first described case of clinically significant resistance to peramivir...
  12. pmc The pharmacological properties of a novel MCH1 receptor antagonist isolated from combinatorial libraries
    Hiroshi Nagasaki
    Dept of Metabolic Medicine, School of Medicine, Nagoya University, Nagoya, Japan
    Eur J Pharmacol 602:194-202. 2009
    ..These results also illustrate the successful application of combinatorial library screening to identify specific surrogate antagonists in an academic setting...
  13. ncbi Characterization of multidrug-resistant influenza A/H3N2 viruses shed during 1 year by an immunocompromised child
    Mariana Baz
    Research Center in Infectious Diseases of the Centre Hospitalier Universitaire de Québec and Laval University, Quebec City, G1V 4G2, Canada
    Clin Infect Dis 43:1555-61. 2006
    ..Development of influenza drug resistance is an important problem in immunocompromised children that could result in treatment failure and viral transmission to others...
  14. pmc Exploiting the mitochondrial unfolded protein response for cancer therapy in mice and human cells
    Markus D Siegelin
    Prostate Cancer Discovery and Development Program, Philadelphia, Pennsylvania, USA
    J Clin Invest 121:1349-60. 2011
    ..Disabling this general adaptive pathway could potentially be used in treatment of genetically heterogeneous human tumors...
  15. pmc Intravenous peramivir for treatment of influenza A and B virus infection in high-risk patients
    Shigeru Kohno
    Second Department of Internal Medicine, Nagasaki University School of Medicine, 1 7 1 Sakamoto, Nagasaki 852 8501, Japan
    Antimicrob Agents Chemother 55:2803-12. 2011
    ..Drug accumulation with repeated doses was thus considered to be of little concern. Intravenous peramivir appears to offer a potentially useful treatment for high-risk patients in the future...
  16. pmc Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir
    S Bantia
    BioCryst Pharmaceuticals, Inc, Birmingham, Alabama 35244, USA
    Antimicrob Agents Chemother 45:1162-7. 2001
    ..No drug-related toxicity was observed in mice receiving 100 mg/kg/day of RWJ-270201 for 5 days. These efficacy and safety profiles justify further consideration of RWJ-270201 for the treatment and prevention of human influenza...
  17. pmc The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors
    Mark Watson
    Gemin X Pharmaceuticals Canada Inc, 3576 Avenue du Parc, Suite 4310, Montreal, Quebec, Canada
    Mol Cell Biol 29:5872-88. 2009
    ..This provides the rationale for a novel therapeutic approach for the use of GMX1777 in the treatment of human cancers...
  18. ncbi Desensitizing and non-desensitizing subtypes of alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in cockroach neurons
    Vincent L Salgado
    Bayer CropScience AG, Global Biology Insecticides, Alfred Nobel Strasse 50, D 40789 Monheim am Rhein, Germany
    J Insect Physiol 50:867-79. 2004
    ..Spinosyn A weakly antagonizes nAChD receptors -23% at 10 microM. The roles of the two nAChR subtypes in insecticide poisoning are discussed...
  19. pmc Mechanism by which mutations at his274 alter sensitivity of influenza a virus n1 neuraminidase to oseltamivir carboxylate and zanamivir
    Michael Z Wang
    Gilead Sciences, Inc, Foster City, California 94404, USA
    Antimicrob Agents Chemother 46:3809-16. 2002
    ..These data indicate that the volume occupied by the amino acid side chain at position 274 can influence the sensitivities of influenza N1 NA but not of N2 NA to both oseltamivir carboxylate and zanamivir...
  20. ncbi Na+/H+ exchanger-1 inhibitors decrease myocardial superoxide production via direct mitochondrial action
    Carolina D Garciarena
    Centro de Investigaciones Cardiovasces, Facultad de Ciencias Medicas, UNLP 60 y 120, 1900 La Plata, Argentina
    J Appl Physiol (1985) 105:1706-13. 2008
    ..Further studies are needed to clarify the precise mechanism and site of action of these drugs in blunting MPTP formation and ROS release...
  21. ncbi Exposure to clothianidin seed-treated canola has no long-term impact on honey bees
    G Christopher Cutler
    Department of Environmental Biology, Ontario Agricultural College, University of Guelph, Guelph, Ontario, Canada N1G 2W1
    J Econ Entomol 100:765-72. 2007
    ..The results show that honey bee colonies will, in the long-term, be unaffected by exposure to clothianidin seed-treated canola...
  22. pmc Investigation of gastrin-releasing peptide as a mediator for 5'-guanidinonaltrindole-induced compulsive scratching in mice
    Saadet Inan
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Peptides 32:286-92. 2011
    ..We conclude that (a) the GRP receptor system does not mediate GNTI-induced scratching and (b) the kappa opioid system is involved, at least in part, in the scratch suppressing activity of nalfurafine...
  23. ncbi Mechanisms of synthetic serine protease inhibitor (FUT-175)-mediated cell death
    Tadashi Uwagawa
    Department of Surgical Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer 109:2142-53. 2007
    ....
  24. ncbi Characterization of sabiporide, a new specific NHE-1 inhibitor exhibiting slow dissociation kinetics and cardioprotective effects
    Nicolas Touret
    Laboratoire de Physiologie Cellulaire et Moleculaire, CNRS UMR6548, Universite de Nice Sophia Antipolis, Faculte des Sciences, Parc Valrose, 06108 cedex 2, Nice, France
    Eur J Pharmacol 459:151-8. 2003
    ..Thus, sabiporide, which possesses remarkable cardioprotective properties, is a specific NHE-1 inhibitor possessing unique binding kinetics...
  25. ncbi Pancreatic proteases and inflammatory mediators in peritoneal fluid during splanchnic arterial occlusion and reperfusion
    Kei Ishimaru
    Second Department of Surgery, Hamamatsu University School of Medicine, Hamamatsu, Japan
    Shock 22:467-71. 2004
    ....
  26. ncbi Interaction between NO and COX pathways in retinal cells exposed to elevated glucose and retina of diabetic rats
    Yunpeng Du
    Clinical and Molecular Endocrinology, Dept of Medicine, 434 Biomedical Research Bldg, Case Western Reserve Univ, 10900 Euclid Ave, Cleveland, OH 44106 4951, USA
    Am J Physiol Regul Integr Comp Physiol 287:R735-41. 2004
    ....
  27. ncbi Mechanisms of protection of the ischemic and reperfused myocardium by sodium-hydrogen exchange inhibition
    M Karmazyn
    Department of Pharmacology and Toxicology, University of Western Ontario, London, Ontario, Canada
    J Thromb Thrombolysis 8:33-8. 1999
    ..Coupled with the low potential for toxicity of the agents, Na-H exchange inhibition could emerge as an effective therapeutic strategy in cardiac disorders, particularly involving conditions associated with ischemia and reperfusion...
  28. pmc Effects of creatine and β-guanidinopropionic acid and alterations in creatine transporter and creatine kinases expression in acute seizure and chronic epilepsy models
    Dae Won Kim
    Department of Biomedical Sciences, College of Life Science, Hallym University, Chunchon Kangwon Do 200 702, Republic of Korea
    BMC Neurosci 11:141. 2010
    ....
  29. pmc Antagonist action of progesterone at σ-receptors in the modulation of voltage-gated sodium channels
    Molly Johannessen
    Department of Physiology, University of Wisconsin School of Medicine and Public Health, Madison, WI 53706, USA
    Am J Physiol Cell Physiol 300:C328-37. 2011
    ....
  30. ncbi Effect of GNTI, a kappa opioid receptor antagonist, on MK-801-induced hyperlocomotion and stereotypy in mice
    Chun ting Qi
    Research Center for Biotechnology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200233, China
    Acta Pharmacol Sin 27:1401-8. 2006
    ....
  31. pmc Impairment of PGC-1alpha expression, neuropathology and hepatic steatosis in a transgenic mouse model of Huntington's disease following chronic energy deprivation
    Rajnish K Chaturvedi
    Department of Neurology and Neuroscience, Weill Medical College of Cornell University, New York, NY 10065, USA
    Hum Mol Genet 19:3190-205. 2010
    ....
  32. ncbi Muscle-specific differences in the response of mitochondrial proteins to beta-GPA feeding: an evaluation of potential mechanisms
    Deon B Williams
    Alberta Diabetes Institute, 4126C HRIF East, Univ of Alberta, Edmonton, Alberta, Canada T6G 2E1
    Am J Physiol Endocrinol Metab 296:E1400-8. 2009
    ..The lack of an effect of beta-GPA feeding on mitochondrial proteins in the soleus muscles could be related to a fiber type-specific effect of beta-GPA on RIP140 protein content...
  33. ncbi Galactosylated multimodular lipoplexes for specific gene transfer into primary hepatocytes
    Emilie Letrou-Bonneval
    INSERM, U533, F 44000 Nantes, France
    J Gene Med 10:1198-209. 2008
    ..Numerous synthetic cationic vectors have been synthesized and are successfully used for in vitro gene transfer but an excess of positive charges can lead to cytotoxicity and does not enable specific transfection...
  34. ncbi The endothelin receptor antagonist CPU0213 is more effective than aminoguanidine to attenuate isoproterenol-induced vascular abnormality by suppressing overexpression of NADPH oxidase [correction of oxidas], ETA, ETB, and MMP9 in the vasculature
    Jin Xu
    Research Division of Pharmacology, China Pharmaceutical University, Nanjing, China
    J Cardiovasc Pharmacol 52:42-8. 2008
    ....
  35. ncbi Creatine transporter activity and content in the rat heart supplemented by and depleted of creatine
    Ernest Boehm
    Wellcome Trust Centre for Human Genetics, University of Oxford, Oxford OX3 7BN, United Kingdom
    Am J Physiol Endocrinol Metab 284:E399-406. 2003
    ..We conclude that, in heart, creatine transport is determined by the content of a plasma membrane isoform of the CrT but not by the total cellular CrT pool...
  36. pmc Early embryo loss is associated with local production of nitric oxide by decidual mononuclear cells
    E K Haddad
    Department of Microbiology and Immunology, McGill University, Montreal, Quebec, Canada
    J Exp Med 182:1143-51. 1995
    ..In addition, aminoguanidine-treated pregnant mice showed a significant increase in average litter size when the pregnancies were allowed to proceed to term.(ABSTRACT TRUNCATED AT 400 WORDS)..
  37. ncbi Randomized trial of an inhibitor of formation of advanced glycation end products in diabetic nephropathy
    W Kline Bolton
    Department of Medicine, University of Virginia Health System, Charlottesville, Va 2908 0133, USA
    Am J Nephrol 24:32-40. 2004
    ..This study was undertaken to determine if pimagedine ameliorates nephropathy in type 1 (insulin-dependent) diabetes mellitus...
  38. ncbi Kinetics and mechanism of the reaction of aminoguanidine with the alpha-oxoaldehydes glyoxal, methylglyoxal, and 3-deoxyglucosone under physiological conditions
    P J Thornalley
    Department of Biological Sciences, University of Essex, Central Campus, Wivenhoe Park, Colchester, United Kingdom
    Biochem Pharmacol 60:55-65. 2000
    ..This effect is limited, however, by the rapid renal elimination of AG. Decreased AGE formation is implicated in the prevention of microvascular complications of diabetes by AG...
  39. ncbi Identification of a binding site on Hsc70 for the immunosuppressant 15-deoxyspergualin
    S G Nadler
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 80543, USA
    Biochem Biophys Res Commun 253:176-80. 1998
    ..These results suggest that in addition to the ATP binding domain, there are two additional substrate binding domains on Hsc70. DSG should provide a tool for understanding the role of the EEVD motif in biological processes...
  40. ncbi Effects of sabiporide, a specific Na+/H+ exchanger inhibitor, on neuronal cell death and brain ischemia
    Hye Seong Park
    Department of Physiology, School of Medicine, Ajou University, Suwon, Kyungkido 442 749, Republic of Korea
    Brain Res 1061:67-71. 2005
    ..In in vivo brain ischemia model, sabiporide produced protective effects, decreasing the infarct size and edema volume. Our results suggest that sabiporide elicits neuroprotective effect both in vitro and in vivo...
  41. pmc Phase III randomized, double-blind study comparing single-dose intravenous peramivir with oral oseltamivir in patients with seasonal influenza virus infection
    Shigeru Kohno
    Second Department of Internal Medicine, Nagasaki University School of Medicine, Nagasaki, Japan
    Antimicrob Agents Chemother 55:5267-76. 2011
    ..Thus, a single intravenous dose of peramivir may be an alternative to a 5-day oral dose of oseltamivir for patients with seasonal influenza virus infection...
  42. pmc Structural and functional basis of resistance to neuraminidase inhibitors of influenza B viruses
    Aaron J Oakley
    CSIRO Materials Science and Engineering, Parkville, 343 Royal Parade, Parkville, Victoria, 3052, Australia
    J Med Chem 53:6421-31. 2010
    ..Lack of the E275 rotation would also account for the loss of slow binding and the partial resistance of influenza B wild type NAs to oseltamivir...
  43. ncbi Nafamostat mesilate is an extremely potent inhibitor of human tryptase
    Shuji Mori
    Department of Pharmacology, Okayama University Graduate School of Medicine and Dentistry, Okayama, Japan
    J Pharmacol Sci 92:420-3. 2003
    ..1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition...
  44. ncbi Effects of clothianidin on Bombus impatiens (Hymenoptera: Apidae) colony health and foraging ability
    Michelle T Franklin
    Department of Biological Sciences, Simon Fraser University, Burnaby, British Columbia, Canada V5A 1S6
    J Econ Entomol 97:369-73. 2004
    ..These results suggest that clothianidin residues found in seed-treated canola and possibly other crops will not adversely affect the health of bumble bee colonies or the foraging ability of workers...
  45. ncbi The hydantoin lesions formed from oxidation of 7,8-dihydro-8-oxoguanine are potent sources of replication errors in vivo
    Paul T Henderson
    Biological Engineering Division and Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA
    Biochemistry 42:9257-62. 2003
    ..Were these lesions to be formed in vivo, our data show that they are absolutely miscoding and may be refractory to repair after translesion synthesis...
  46. pmc A self-cleaving DNA enzyme modified with amines, guanidines and imidazoles operates independently of divalent metal cations (M2+)
    Marcel Hollenstein
    Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver BC, V6T 1Z1, Canada
    Nucleic Acids Res 37:1638-49. 2009
    ....
  47. ncbi Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines
    Paul V Fish
    Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent, CT13 9NJ, UK
    J Med Chem 50:2341-51. 2007
    ..On the basis of this profile, compound 26 (UK-371,804) was selected as a candidate for further preclinical evaluation for the treatment of chronic dermal ulcers...
  48. ncbi Influence of aminoguanidine, an inhibitor of inducible nitric oxide synthase, on the pulmonary hypertensive response to microparticle injections in broilers
    R F Wideman
    Department of Poultry Science, University of Arkansas, Fayetteville 72701, USA
    Poult Sci 85:511-27. 2006
    ..Different NOS-mediated responses among broiler populations may affect pulmonary hemodynamic characteristics of broiler lines selected using i.v. microparticle injections...
  49. ncbi Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys
    S Stevens Negus
    Alcohol and Drug Abuse Research Center, Harvard Medical School, McLean Hospital, 115 Mill Street, Belmont, MA 02478, USA
    Psychopharmacology (Berl) 163:412-9. 2002
    ..Receptor-selective antagonists are useful experimental tools for evaluation of opioid receptor-mediated processes. 5'-Guanidinonaltrindole (GNTI) was recently developed as a novel kappa-selective antagonist...
  50. ncbi Catalytic addition of alkyne C-H, amine N-H, and phosphine P-H bonds to carbodiimides: an efficient route to propiolamidines, guanidines, and phosphaguanidines
    Wen Xiong Zhang
    Organometallic Chemistry Laboratory, RIKEN The Institute of Physical and Chemical Research, Hirosawa 2 1, Wako, Saitama 351 0198, Japan
    Org Biomol Chem 6:1720-30. 2008
    ..of alkyne C-H, amine N-H, and phosphine P-H bonds to carbodiimides, to give a new family of propiolamidines, guanidines, and phosphaguanidines, some of which were difficult to prepare previously...
  51. ncbi Effect of nitric oxide on phagocytic activity of lipopolysaccharide-induced macrophages: possible role of exogenous L-arginine
    Cemil Tumer
    Department of Physiology, Faculty of Medicine, Mustafa Kemal University, Uur Mumcu Street, 31100 Hatay, Turkey
    Cell Biol Int 31:565-9. 2007
    ..As a result, we showed that NO produced by macrophages has a role not only in intracellular killing, but also in phagocytic activity...
  52. ncbi Comparative in vivo adulticidal activity of a topical dinotefuran versus an imidacloprid-based formulation against cat fleas (Ctenocephalides felis) on cats
    Martin Murphy
    Charles River Laboratories Preclinical Services Ireland, Carrentrila, Ballina, Co Mayo, Ireland
    Vet Ther 10:9-16. 2009
    ..05) fewel fleas than cats treated with imidacloprid on days 0 (2 hours after treatment), 9, 16, 23, 29 (6 and 12 hours after infestation), and 30...
  53. ncbi Effects of inhibition of glycation and oxidative stress on the development of cataract and retinal vessel abnormalities in diabetic rats
    E Agardh
    Department of Ophthalmology, University Hospital MAS, Malmo, Sweden
    Curr Eye Res 21:543-9. 2000
    ..To study effects of inhibition of glycation, and oxidative stress on the development of cataract and retinal vessel abnormalities in diabetic rats...
  54. pmc Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
    Thomas A Munro
    McLean Hospital, Belmont, MA and Department of Psychiatry, Harvard Medical School, Boston, MA, USA
    BMC Pharmacol 12:5. 2012
    ..Recent evidence suggests, instead, that they induce prolonged desensitization of the κ opioid receptor...
  55. ncbi Stimulation of mitochondrial gene expression and proliferation of mitochondria following impairment of cellular energy transfer by inhibition of the phosphocreatine circuit in rat hearts
    R J Wiesner
    Department of Physiology II, University of Heidelberg, Germany
    J Bioenerg Biomembr 31:559-67. 1999
    ..The observed activation of the mtTFA gene corroborates the important function of this protein in nuclear-mitochondrial communication...
  56. ncbi Amidines, isothioureas, and guanidines as nucleophilic catalysts
    James E Taylor
    Department of Chemistry, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Chem Soc Rev 41:2109-21. 2012
    ..Amidines and guanidines are often only thought of as strong organic bases however, a number of small molecules containing basic ..
  57. ncbi Diverse actions of neonicotinoids on chicken alpha7, alpha4beta2 and Drosophila-chicken SADbeta2 and ALSbeta2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes
    Makoto Ihara
    Department of Agricultural Chemistry, Faculty of Agriculture, Kinki University, 3327 204 Nakamachi, Nara 631 8505, Japan
    Neuropharmacology 45:133-44. 2003
    ....
  58. ncbi Evaluation of neonicotinoid, organophosphate and avermectin trunk injections for the management of avocado thrips in California avocado groves
    Frank J Byrne
    Department of Entomology, University of California, Riverside, CA 92521, USA
    Pest Manag Sci 68:811-7. 2012
    ..Residues in fruit were quantified to determine whether trunk injection of insecticides might present a greater risk than traditional application methods for contaminating fruit...
  59. ncbi Efficacy of dinotefuran, permethrin and pyriproxyfen combination spot-on against Aedes aegypti mosquitoes on dogs
    Michel Franc
    Universite de Toulouse, INP, ENVT, F 31076 Toulouse, France
    Vet Parasitol 189:333-7. 2012
    ..No adverse events were observed following treatment, including observations conducted 2, 4 and 24h after the last dog was treated...
  60. pmc Inhibitory effect of lidocaine on pain and itch using formalin-induced nociception and 5'-guanidinonaltrindole-induced scratching models in mice: behavioral and neuroanatomical evidence
    Saadet Inan
    Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA
    Eur J Pharmacol 616:141-6. 2009
    ..Our results highlight the antipruritic properties of lidocaine and argue for its comprehensive clinical testing against pruritic states...
  61. ncbi Structure-activity relationship study on alpha1 adrenergic receptor antagonists from beer
    Toshiyuki Wakimoto
    School of Pharmaceutical Sciences, University of Shizuoka and Global COE Program, 52 1 Yada, Suruga ku, Shizuoka shi, Shizuoka 422 8526, Japan
    Bioorg Med Chem Lett 19:5905-8. 2009
    ..Furthermore, the related, synthetic compound, (2R,3R)-methyl benzofurancarboxylate exhibits antagonist activity against the alpha1A adrenoceptor at a lower concentration than that of hordatine A...
  62. ncbi Efficacy of permethrin, dinotefuran and pyriproxyfen on adult fleas, flea eggs collection, and flea egg development following transplantation of mature female fleas (Ctenocephalides felis felis) from cats to dogs
    E Bouhsira
    Universite de Toulouse, INP, ENVT, F 3107 Ecole Nationale Vétérinaire de Toulouse, 23 Chemin des Capelles, 31079 Toulouse, France
    Vet Parasitol 190:541-6. 2012
    ..20%, p<0.05). The egg laying inhibition was over 92.3% for up to 29 days (p<0.05). The adult emergence inhibition remained 100% during 8 weeks after treatment and was 99.8% nine weeks after treatment (p<0.001)...
  63. ncbi Chemical and pharmacological significance of natural guanidines from marine invertebrates
    S S Ebada
    Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University, Universitaetsstrasse 1, D 40225 Duesseldorf, Germany
    Mini Rev Med Chem 11:225-46. 2011
    Natural Guanidines from marine invertebrates represent a group of bioactive secondary metabolites that revealed prominent pharmacological activities such as antimicrobial, antiproliferative, analgesic, and anti-coagulant properties...
  64. ncbi Na(+)/H(+) exchange inhibition with HOE642 improves postischemic recovery due to attenuation of Ca(2+) overload and prolonged acidosis on reperfusion
    H Strömer
    Medizinische Universitatsklinik, Wurzburg, Germany
    Circulation 101:2749-55. 2000
    ..Attenuated Ca(2+) overload and prolonged acidosis are known to be cardioprotective...
  65. pmc Quantitation of four guanine oxidation products from reaction of DNA with varying doses of peroxynitrite
    Hongbin Yu
    Biological Engineering Division, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Room 56 731A, Cambridge, Massachusetts 02139, USA
    Chem Res Toxicol 18:1849-57. 2005
    ..The complexity of these dose-response relationships is likely due to the dual role of peroxynitrite as both an oxidant and a nucleophile in competition with water...
  66. pmc Efficacy, safety, and pharmacokinetics of intravenous peramivir in children with 2009 pandemic H1N1 influenza A virus infection
    Norio Sugaya
    Department of Pediatrics, Keiyu Hospital, Yokohama, Japan
    Antimicrob Agents Chemother 56:369-77. 2012
    ....
  67. pmc Anti-inflammatory activity of creatine supplementation in endothelial cells in vitro
    Akihiro Nomura
    Department of Pulmonary Medicine, Institute of Clinical Medicine, University of Tsukuba, Tennoudai 1 1 1, Tsukuba, Ibaraki 305 8575, Japan
    Br J Pharmacol 139:715-20. 2003
    ..7 The present study suggests that CR supplementation has anti-inflammatory activities against endothelial cells...
  68. ncbi Advanced glycation end product interventions reduce diabetes-accelerated atherosclerosis
    Josephine M Forbes
    Danielle Alberti Memorial Centre for Diabetes Complications, Vascular Division, Wynn Domain, Baker Medical Research Institute, Melbourne, Australia
    Diabetes 53:1813-23. 2004
    ..Attenuation of these changes was seen in both treated diabetic groups. ALT-711 and AG demonstrated the ability to reduce vascular AGE accumulation in addition to attenuating atherosclerosis in these diabetic mice...
  69. ncbi Chronic phosphocreatine depletion by the creatine analogue beta-guanidinopropionate is associated with increased mortality and loss of ATP in rats after myocardial infarction
    M Horn
    Medizinische Universitatsklinik, Wurzburg University, Germany
    Circulation 104:1844-9. 2001
    ..In the present study, myocardial PCr stores in a heart failure model were further depleted by feeding of the PCr analogue beta-guanidinopropionate (GP). Functional and metabolic consequences were studied...
  70. pmc Inhibition of Na+/H+-exchanger with sabiporide attenuates the downregulation and uncoupling of the myocardial beta-adrenoceptor system in failing rabbit hearts
    Kirsten Leineweber
    Institute of Pathophysiology, University of Essen School of Medicine, D 45122 Essen, Germany
    Br J Pharmacol 148:137-46. 2006
    ..Accordingly, additional studies are needed to fully establish the cause-and-effect relationship between NHE-1 inhibition and the restoration of the myocardial betaAR system...
  71. ncbi Modification of intracellular calcium concentration in cardiomyocytes by inhibition of sarcolemmal Na+/H+ exchanger
    Harjot K Saini
    Institute of Cardiovascular Sciences, St Boniface General Hospital Research Centre, University of Manitoba, Winnipeg, MB, Canada R2H 2A6
    Am J Physiol Heart Circ Physiol 291:H2790-800. 2006
    ....
  72. ncbi Role of nitric oxide on pathogenesis of 5-fluorouracil induced experimental oral mucositis in hamster
    R F C Leitão
    Departamento de Fisiologia e Farmacologia, Faculdade de Medicina da Universidade Federal do Ceará, Rua Cel Nunes de Melo, 1127, 60 430 270 Fortaleza, CE, Brazil
    Cancer Chemother Pharmacol 59:603-12. 2007
    ..Mucositis induced by antineoplastic drugs is an important, dose-limiting, and costly side effect of cancer therapy. Aim: To investigate the role of nitric oxide (NO) on the pathogenesis of 5-fluorouracil (5-FU)-induced oral mucositis...
  73. ncbi Effect of aminoguanidine on ischemia-reperfusion induced myocardial injury in rats
    Hakan Parlakpinar
    Department of Pharmacology, Faculty of Medicine, Inonu University, Malatya, Turkey
    Mol Cell Biochem 277:137-42. 2005
    ..In conclusion, this study indicates that iNOS inhibitor, AMG, show reduction in NO's side effect in I/R injury...
  74. pmc GPA protects the nigrostriatal dopamine system by enhancing mitochondrial function
    Tamas L Horvath
    Section of Comparative Medicine, Yale University School of Medicine, New Haven, CT 06520, USA
    Neurobiol Dis 43:152-62. 2011
    ..Mitochondrial dysfunction is a common problem in neurodegeneration and thus GPA may slow disease progression in other models of neurodegeneration...
  75. ncbi Effects of the creatine analogue beta-guanidinopropionic acid on skeletal muscles of mice deficient in muscle creatine kinase
    J van Deursen
    Department of Cell Biology and Histology, Faculty of Medical Sciences, University of Nijmegen, The Netherlands
    Biochim Biophys Acta 1185:327-35. 1994
    ..Altogether, these results provide evidence that certain functions of the creatine kinase/phosphocreatine (CK/PCr) system are not eliminated solely by the loss of M-CK...
  76. ncbi Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies
    P K Jadhav
    Chemical and Physical Sciences Department, The DuPont Merck Pharmaceutical Company, Experimental Station, P O Box 80500, Wilmington, Delaware 19880 0500, USA
    J Med Chem 41:1446-55. 1998
    ..The choice of cyclic cyanoguanidines over cyclic guanidines was based on the reduced basicity of the former...
  77. ncbi Nafamostat mesilate inhibits high-mobility group box 1 by lipopolysaccharide stimulation in murine macrophage RAW 264.7
    Satoshi Hagiwara
    Department of Brain and Nerve Science, Anesthesiology, Oita University Faculty of Medicine, Yufu City, Oita, Japan
    Shock 27:429-35. 2007
    ..Our findings thus suggest that the administration of NM may therefore potentially improve the condition of patients who have septic shock...
  78. ncbi Serine proteases are involved in the pathogenesis of trauma-hemorrhagic shock-induced gut and lung injury
    Edwin A Deitch
    Department of Surgery, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, New Jersey 07103, USA
    Shock 19:452-6. 2003
    ....
  79. ncbi Stimulation of HSP72 expression following ATP depletion and short-term exercise training in fast-twitch muscle
    L Ecochard
    Unite Mixte de Recherche, Centre National de la Recherche Scientifique, Laboratoire de Physiologie, Universite Claude Bernard, Lyon, France
    Acta Physiol Scand 180:71-8. 2004
    ..In this study, we tested the hypothesis that energy status is a key regulatory event for HSP72 accumulation in skeletal muscles...
  80. ncbi The discovery of dinotefuran: a novel neonicotinoid
    Takeo Wakita
    Life Science Laboratory, Mitsui Chemicals, Inc, 1144 Togo, Mobara, Chiba 297 0017, Japan
    Pest Manag Sci 59:1016-22. 2003
    ..It resulted in dinotefuran which has a (+/-)-tetrahydro-3-furylmethyl moiety instead of a halogenated aromatic heterocyclic ring, and belongs to the third-generation neonicotinoids (sub-class: furanicotinyl compounds)...
  81. ncbi An in vivo approach for globally estimating the drug flow between blood and tissue for nafamostat mesilate: the main hydrolysis site determination in human
    Yan Guang Cao
    Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, PR China
    Biol Pharm Bull 31:1985-9. 2008
    ..The relative hydrolysis fraction indicated that the main hydrolysis site in human body may locate in tissue, which was different to rats...
  82. ncbi Complement inhibitor prevents disruption of sodium channel clusters in a rabbit model of Guillain-Barré syndrome
    Vongsavanh Phongsisay
    Department of Neurology, Dokkyo Medical University, Kitakobayashi 880, Mibu, Shimotsuga, Tochigi 321 0293, Japan
    J Neuroimmunol 205:101-4. 2008
    ..Nafamostat mesilate inhibited complement deposition and prevented sodium channel disruption. This provided the rationale for a clinical trial...
  83. pmc Effects of moderate hypothermia on sarcolemmal Na(+)/H(+) exchanger activity and its inhibition by cariporide in cardiac ventricular myocytes
    K Hoshino
    Centre for Cardiovascular Biology and Medicine, King's College London, London SE1 7EH, UK
    Br J Pharmacol 134:1587-95. 2001
    ..6. We conclude that moderate hypothermia produces (1) a significant, but partial, inhibition of sarcolemmal NHE activity, and (2) no significant effect on the NHE-inhibitory potency of cariporide...
  84. ncbi Decreasing intramuscular phosphagen content simultaneously increases plasma membrane FAT/CD36 and GLUT4 transporter abundance
    Kristin E Pandke
    Dept of Human Health and Nutritional Sciences, Univ of Guelph, Guelph, Ontario, Canada N1G 2W1
    Am J Physiol Regul Integr Comp Physiol 295:R806-13. 2008
    ..Thus the content of sarcolemmal transporters for both of the major energy substrates for muscle increased in response to a reduced energy charge. Increased phosphorylation of AMPK may be one of the triggers for this response...
  85. ncbi Molecular modeling study and synthesis of novel dicationic flexible triaryl guanidines and imidamides as antiprotozoal agents
    Reem K Arafa
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El Aini St, 11562, Cairo, Egypt
    Eur J Med Chem 46:5852-60. 2011
    A new series of fourteen dicationic flexible triaryl bis-guanidines 3a,b, bis-N-substituted guanidines 7a,b and 8a,b as well as bis-imidamides 9-12a,b having a 1,3- or 1,4-diphenoxybenzene scaffold backbone were synthesized...
  86. ncbi Protective effect of aminoguanidine against nephrotoxicity induced by amikacin in rats
    H Parlakpinar
    Department of Pharmacology, Faculty of Medicine, Inonu University, 44069, Malatya, Turkey
    Urol Res 32:278-82. 2004
    ..In addition, AG reversed the morphological damage to the kidney induced by AK. The results show that AG has a protective effect on nephrotoxicity induced by AK and may therefore improve the therapeutic index of AK...
  87. ncbi Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists
    CHRISTOPHER SINZ
    Discovery and Preclinical Sciences, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 21:7131-6. 2011
    ..One compound was orally efficacious in a murine glucagon challenge pharmacodynamic model and also significantly lowered glucose levels in a murine diabetes model...
  88. ncbi Spiroiminodihydantoin and guanidinohydantoin are the dominant products of 8-oxoguanosine oxidation at low fluxes of peroxynitrite: mechanistic studies with 18O
    Jacquin C Niles
    Biological Engineering Division and Department of Chemistry, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Room 56 738A, Cambridge, Massachusetts 02139, USA
    Chem Res Toxicol 17:1510-9. 2004
    ..To explain the pH-dependent Gh and Sp yields, we propose that 5 has a pKa approximately 5.8 and that the differential reactivity of the protonated and deprotonated form of 5 leads to its partitioning into Gh and Sp, respectively...
  89. ncbi Antihyperglycemic action of guanidinoalkanoic acids: 3-guanidinopropionic acid ameliorates hyperglycemia in diabetic KKAy and C57BL6Job/ob mice and increases glucose disappearance in rhesus monkeys
    M D Meglasson
    Metabolic Diseases Research, Upjohn Company, Kalamazoo, Michigan
    J Pharmacol Exp Ther 266:1454-62. 1993
    To evaluate the long-held concept that acidic guanidines lack glycemic effects, guanidinoalkanoic acids and the biguanide metformin (positive control) were administered to KKAy mice, a model of noninsulin-dependent diabetes...
  90. ncbi An inhibitor of inducible nitric oxide synthase and scavenger of peroxynitrite prevents diabetes development in NOD mice
    W L Suarez-Pinzon
    Department of Medicine, University of Alberta, Edmonton, Alberta, Canada
    J Autoimmun 16:449-55. 2001
    ..These findings indicate that both superoxide and nitric oxide radicals contribute to islet beta-cell destruction in autoimmune diabetes via peroxynitrite formation in the beta-cells...
  91. ncbi The orally active antihyperglycemic drug beta-guanidinopropionic acid is transported by the human proton-coupled amino acid transporter hPAT1
    Linda Metzner
    Martin Luther University Halle Wittenberg, Halle, Germany
    Mol Pharm 6:1006-11. 2009
    ..Moreover, with beta-GPA we identified a new high affinity hPAT1 substrate that might be an interesting starting point for future drug design-drug delivery strategies...
  92. ncbi The sigma agonist 1,3-di-o-tolyl-guanidine directly blocks SK channels in dopaminergic neurons and in cell lines
    Cedric Lamy
    Laboratory of Pharmacology, GIGA Neurosciences, University of Liege, B 4000 Sart Tilman Liège 1, Belgium
    Eur J Pharmacol 641:23-8. 2010
    ..This action was also unaffected by BD 1047. Other sigma receptor ligands had little or no effect. We conclude that DTG directly blocks SK channels. This pharmacological action may be important to consider in future experimental settings...
  93. ncbi Analytical evaluation of enzyme-linked immunosorbent assay for neonicotinoid dinotefuran for potential application to quick and simple screening method in rice samples
    Eiki Watanabe
    National Institute for Agro Environmental Sciences, Tsukuba, Ibaraki 305 8604, Japan
    Talanta 84:1107-11. 2011
    ..98). These findings strongly indicate that the evaluated and validated ELISA has a potential utility in a quick, simple, and reliable residue analysis, especially a screening method before shipment contributing to food safety...
  94. pmc Differential effects of endurance training and creatine depletion on regional mitochondrial adaptations in rat skeletal muscle
    D Roussel
    Laboratoire de Physiologie des Régulations Energétiques, Cellulaires et Moleculaires, UMR 5578 CNRS, 8 avenue Rockefeller, 69373 Lyon Cedex 08, France
    Biochem J 350:547-53. 2000
    ..It therefore seems that endurance training and feeding with GPA, which are both known to alter the energetic status of the muscle cell, might mediate distinct biochemical adaptations in regional skeletal muscle mitochondria...
  95. pmc Efficacy and safety of intravenous peramivir for treatment of seasonal influenza virus infection
    Shigeru Kohno
    2nd Department of Internal Medicine, Nagasaki University School of Medicine, 1 7 1 Sakamoto, Nagasaki, Japan
    Antimicrob Agents Chemother 54:4568-74. 2010
    ..Peramivir was well tolerated, and its adverse-event profile was similar to that of placebo. A single intravenous dose of peramivir is effective and well tolerated in subjects with uncomplicated seasonal influenza virus infection...
  96. ncbi Impact of zanamivir on antibiotic use for respiratory events following acute influenza in adolescents and adults
    L Kaiser
    University of Virginia School of Medicine, Department of Internal Medicine, Division of Epidemiology and Virology, Box 800473, Charlottesville, VA 22908, USA
    Arch Intern Med 160:3234-40. 2000
    ..Influenza infections commonly lead to respiratory tract complications that result in antibiotic treatment...
  97. ncbi Anti-influenza virus activity of peramivir in mice with single intramuscular injection
    Shanta Bantia
    Department of Biological Sciences, BioCryst Pharmaceuticals, Inc, 2190 Parkway Lake Drive, Birmingham, AL 35244, USA
    Antiviral Res 69:39-45. 2006
    ..A single intramuscular injection of peramivir may successfully treat influenza infections and provide an alternate option to oseltamivir during an influenza outbreak...
  98. ncbi Randomized, placebo-controlled studies of inhaled zanamivir in the treatment of influenza A and B: pooled efficacy analysis
    A S Monto
    Department of Epidemiology, School of Public Health, University of Michigan, Ann Arbor, USA
    J Antimicrob Chemother 44:23-9. 1999
    ..001). These results highlight the groups likely to show greatest benefit from zanamivir treatment, and confirm the clinical relevance of the treatment benefit...
  99. ncbi Cardiopulmonary bypass using nafamostat mesilate for patients with infective endocarditis and recent intracranial hemorrhage
    Takeyoshi Ota
    Department of Cardiovascular Surgery, Kobe University Graduate School of Medicine, 7 5 2 Kusunoki cho, Chuo Ku, Kobe, 650 0017, Japan
    Interact Cardiovasc Thorac Surg 6:270-3. 2007
    ..In this study, a cardiopulmonary bypass strategy using nafamostat mesilate as an anticoagulant for such patients is discussed based on three cases we experienced...
  100. ncbi Extracorporeal membrane oxygenation with nafamostat mesilate as an anticoagulant for massive pulmonary hemorrhage after living-donor lobar lung transplantation
    Kazutoshi Kotani
    Departments of Oncology and Thoracic Surgery, Emergency Medicine, Cardiovascular Surgery, and Anesthesiology and Resuscitology, Graduate School of Medicine and Dentistry, Okayama University, Okayama, Japan
    J Thorac Cardiovasc Surg 124:626-7. 2002
  101. ncbi Serine protease inhibitor nafamostat given before reperfusion reduces inflammatory myocardial injury by complement and neutrophil inhibition
    Hansjorg Schwertz
    Department of Medicine III, Martin Luther University, Halle, Germany
    J Cardiovasc Pharmacol 52:151-60. 2008
    ..Reduced leukocyte accumulation and complement activity seem involved in the mechanism of this cardioprotective effect...

Research Grants65

  1. Identification of LSD1 inhibitors targeting epigenetic regulation in tumor cells
    Patrick M Woster; Fiscal Year: 2013
    ..We recently reported a series of (bis)guanidines and (bis)biguanides that are potent inhibitors of recombinant human LSD1...
  2. Improving in vivo stability of sphingosine kinase inhibitors
    STEVEN BRANDON THORPE; Fiscal Year: 2012
    ..Herein we outline a set of strategies including pro-drug forms, modified amidines, guanidines, etc. to render the SphK1 inhibitors drug like...
  3. Discovery Based Studies of Medicinally Relevant Pharmacophore Libraries
    Matthew S Sigman; Fiscal Year: 2012
    ..These architectures are broadly identified as 1) diarylmethines;2) 2-aminoimidazoles/cyclic guanidines and 3) dimeric indoles...
  4. PRACTICAL CHEMICAL SYNTHESIS OF COMPLEX ALKALOIDS
    LARRY OVERMAN; Fiscal Year: 2009
    ..of our HL research program is to develop stereo- and enantiocontrolled methods for constructing complex guanidines and other strongly basic molecules...
  5. SMALL MOLECULE ORPHANIN FQ/NOCICEPTIN RECEPTOR LIGANDS
    Richard Houghten; Fiscal Year: 2000
    ..Examples of the heterocyclic libraries include bicyclic guanidines, substitute isoquinilones, indole-imidazoles, quinazolinones, cyclic ureas and hydantoins...
  6. SYNTHETIC NEUROPROTECTIVE GLUTAMATE RELEASE BLOCKERS
    STANLEY GOLDIN; Fiscal Year: 1992
    ..l.'s laboratory, that certain substituted guanidines and related compounds are antagonists of calcium-dependent release of glutamate and dopamine from brain nerve ..
  7. SUBSTITUTED GUANIDINES AS NEUROPROTECTIVE DRUGS
    Robert McBurney; Fiscal Year: 1991
    ..The starting point for this project was our finding that certain substituted guanidines were use-dependent blockers of the cation channel associated with the NMDA receptor...
  8. IDENTIFICATION OF RECEPTOR SPECIFIC OPIOID LIGANDS
    Richard Houghten; Fiscal Year: 2002
    ..molecular weight acyclic and heterocyclic compounds, including indole-imidazoles, quinazolinones, and bicyclic guanidines. The focus of the proposed work will be to use these libraries, as well as libraries of globally fluorescent ..
  9. HIGH AFFINITY AGONISTS OF HIV1 DEPENDENT FUSION
    Sylvie Blondelle; Fiscal Year: 2001
    ..dipeptidomimetics, polyamines, indole-pyrido- imadazoles, N-alkyl amino cyclic ureas and thioureas and bicyclic guanidines) for their ability to inhibit fusogenic activity mediated by HIV-1 recombinant glycoprotein using two assay ..
  10. A NOVEL PEROXYNITRITE SCAVENGER COMPOUND
    Garry Southan; Fiscal Year: 1999
    ..As a next generation of guanidines, Inotek proposes to prepare and test selenoethylguanidine...
  11. Development of PET Radioligands for NMDA Receptors
    Rikki Waterhouse; Fiscal Year: 2004
    ..To identity effective PCP site tracers, novel substituted N, N'-alkyl-diphenyl guanidines will be synthesized and evaluated...
  12. Reducing Transmission of Influenza by Face Masks
    ARNOLD MONTO; Fiscal Year: 2008
    ..Such a reduction could have a major public health impact during a pandemic. In the second year, the study can be expanded or modified based on findings in the first. ..
  13. Comparative Study of Influenza Vaccines in Adults
    ARNOLD MONTO; Fiscal Year: 2006
    ..Results will help to determine how the vaccine may be used as part of the strategy to combat influenza in varying situations. [unreadable] [unreadable]..
  14. Mechanisms of influenza NA drug resistance
    Jennifer L McKimm Breschkin; Fiscal Year: 2010
    ....
  15. New Methodology for Indole Alkaloid Syntheses
    Ken S Feldman; Fiscal Year: 2010
    ..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
  16. Alkynyliodonium Salts and Derived Diyls in Synthesis
    Ken Feldman; Fiscal Year: 2009
    ..abstract_text> ..
  17. MICROVASCULAR INJURY DURING EXTRACORPOREAL LIFE SUPPORT
    Charles Cox; Fiscal Year: 2004
    ..Dr. McIntire's expertise in PMN/endothelial/blood flow interactions will provide an important addition to the candidate's training. ..
  18. MIBG ANALOGUE RADIOPHARMACEUTICALS
    Ganesan Vaidyanathan; Fiscal Year: 2001
    ..Strategies to augment tumor-to-normal tissue ratios will be investigated. The outcome of this study should help improve the endoradiotherapy of neuroendocrine tumors and possibly of medulloblastoma. ..
  19. Hypothermia for Acute Brain Injury in Children
    Charles Cox; Fiscal Year: 2004
    ..abstract_text> ..
  20. Chemical and Biological Studies on Biaryl Phenolics
    Ken Feldman; Fiscal Year: 2005
    ..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
  21. Imaging of O6-Alkylguanine-DNA Alkyltransferase
    Ganesan Vaidyanathan; Fiscal Year: 2005
    ..In summary, this proposal seeks to determine whether the development of a suitable agent for the imaging of tumor AGT will facilitate chemotherapy planning, thereby improving the outcome of alkylator chemotherapy. ..
  22. NOVEL NONPEPTIDE LIGANDS FOR THE OPIOID RECEPTORS
    Subramaniam Ananthan; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  23. MOLECULAR MECHANISMS OF LUNG SURFACTANT SECRETION
    Lin Liu; Fiscal Year: 2007
    ..Accomplishing the goals of this proposal will give a valuable direction to the therapy of pulmonary diseases such as neonatal respiratory distress syndrome. ..
  24. MEMBRANE EXCITABILITY AND SECRETION FROM NERVE ENDINGS
    Meyer Jackson; Fiscal Year: 2007
    ....
  25. M.tuberculosis Rpfs: Modulators of Reactivation
    JoAnn Tufariello; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  26. Hematopoietic Stem Cell Therapy for Myocardial Regeneration
    Roberto Bolli; Fiscal Year: 2007
    ..The results may eventually lead to the development of novel therapeutic strategies in patients with ischemic heart disease. ..
  27. Biochemical and Behavioral Mechanisms of Toxicology
    JACK HINSON; Fiscal Year: 2006
    ..By training students over this continuum the investigators will add a pool of toxicologists capable of addressing our national needs. ..
  28. AGMATINASE INHIBITORS FOR HYPOXIC-ISCHEMIC NEW BORN BRAIN DAMAGE
    John Piletz; Fiscal Year: 2007
    ..The overall goal of these studies is to develop a treatment for perinatal brain damage in human infants. [unreadable] [unreadable] [unreadable]..
  29. TRANSGENIC/KNOCKOUT ANIMALS IN MYOCARDIAL PRESERVATION
    DIPAK DAS; Fiscal Year: 2008
    ..The results of this proposed research will hopefully increase our understanding of redox regulation by Trx/Grx in the ischemic myocardium. [unreadable] [unreadable]..
  30. Pulmonary Arterial Hypertension: Avian Model of Complex Vascular Lesion Developme
    ROBERT WIDEMAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  31. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  32. NMDA Receptor Dynamics After Brain Injury
    Anat Biegon; Fiscal Year: 2011
    ..The results may explain the failure of NMDAR antagonists in clinical trials and suggest novel strategies for treatment of brain injury. ..
  33. Design of peptide entry inhibitors and delivery systems to target emerging henipa
    Anne Moscona; Fiscal Year: 2010
    ..abstract_text> ..
  34. Design of peptide entry inhibitors and delivery systems to target emerging henipa
    Anne Moscona; Fiscal Year: 2008
    ..abstract_text> ..
  35. Hepcidin and the pathogenesis of anemia in older adults.
    Richard D Semba; Fiscal Year: 2010
    ..This study should provide new insight into the epidemiology and biological mechanisms of anemia among older adults and help identify strategies aimed at the prevention and treatment of anemia. ..
  36. Mechanisms of Alveolar Fluid Transport
    Lin Liu; Fiscal Year: 2009
    ..An understanding of the mechanisms of fluid transport in the lung will provide valuable insights and directions toward therapeutic intervention in fetal lung diseases and the resolution of pulmonary edema. ..
  37. Iron Deficiency and Anemia in HIV and HCV-Infected Women
    Richard Semba; Fiscal Year: 2005
    ..S. and elsewhere. ..
  38. HEART IMAGING AGENTS--STRUCTURAL MECHANISTICS STUDY
    David Raffel; Fiscal Year: 2004
    ..Finally, [11C]- and [18F]-labeled polar derivatives of the psychostimulant methcathinone will be synthesized as potential NET markers and their in vitro NET affinities determined as the cloned human NET transporter. ..
  39. ANTI-VIRAL TREATMENT OF DEVELOPING BOVINE EMBRYOS
    Maurice Givens; Fiscal Year: 2002
    ....
  40. NEPHRITOGENIC EPITOPES IN GOODPASTURES SYNDROME
    WARREN BOLTON; Fiscal Year: 2001
    ..Further, the knowledge resultant from these investigations may provide a basis for the eventual development of specific therapeutic interventions for Goodpasture's syndrome. ..
  41. MR STUDIES OF EXPERIMENTAL RETINOPATHY OF PREMATURITY
    BRUCE BERKOWITZ; Fiscal Year: 2001
    ..This work may have broad impact beyond ROP since abnormal blood vessel growth is a common pathobiologic event for other blinding disorders, such as diabetic retinopathy. ..
  42. Oxidative Stress and Hemodialysis Access Failure
    MIRIAM WEISS; Fiscal Year: 2002
    ..Specific Aim C: To compare the success rates of prophylactic angioplasty when non-invasive techniques demonstrate decreased flow in the hemodialysis access in alpha-tocopherol-treated versus placebo-treated patients. ..
  43. PATHOLOGICAL MECHANISMS OF DEMYELINATION
    Thomas Lane; Fiscal Year: 2002
    ..Together, these studies will provide insight into the complex immunological mechanisms involved in CNS demyelinating disease and allow a better understanding of the pathological mechanisms which exist in human demyelinating disease. ..
  44. MYOCARDIAL CALCIUM HANDLING DURING AND AFTER HYPOTHERMIA
    DAVID STOWE; Fiscal Year: 2002
    ..These studies will lead to a better understanding of Ca2+ loading and therapies to protect hypothermic hearts. ..
  45. PEROXYNITRITE IN ACETAMINOPHEN INDUCED HEPATOTOXICITY
    JACK HINSON; Fiscal Year: 2002
    ..By understanding the role of peroxynitrite in acetaminophen hepatotoxicity, new treatment paradigms may be developed for hepatotoxicity, and this mechanism may be important with other toxins. ..
  46. IMIDAZOLINE RECEPTORS IN DEPRESSION--BASIC STUDIES
    John Piletz; Fiscal Year: 2001
    ..The findings from the clinical grant will best be understood within the context of these studies in the basic grant, and vice versa. ..
  47. EFFECT OF COMP MUTATION ON MUSCULOSKELETAL DEVELOPMENT
    Paul Di Cesare; Fiscal Year: 2002
    ..Identifying the functions, synthesis, interactions, tissue distribution and expression of COMP is critical to understanding its influence on growth during endochondral ossification and articular cartilage structure and function. ..
  48. OXYGEN RADICALS AND POSTISCHEMIC DYSFUNCTION
    Roberto Bolli; Fiscal Year: 2002
    ..Elucidation of the mechanism of late PC should facilitate the development of drugs that duplicate its powerful cardioprotective effects. ..
  49. MMP-9-Dependent Vessel Wall Remodeling is NO-Dependent
    Gilbert Upchurch; Fiscal Year: 2005
    ....
  50. Two-Photon Microscope Patch Clamp Integrated System
    Meyer Jackson; Fiscal Year: 2005
    ..abstract_text> ..
  51. Behavioral Influences on Drug Tolerance
    James Smith; Fiscal Year: 2005
    ..Additionally, "multi-chamber" procedures will study generalization of those discriminative effects to performance of the same subjects in different circumstances. ..
  52. ADJUNCT VITAMIN A THERAPY FOR TUBERCULOSIS AND HIV/AIDS
    Richard Semba; Fiscal Year: 2005
    ....
  53. IMAGING EPILEPTIFORM ACTIVITY IN PIRIFORM CORTEX
    Meyer Jackson; Fiscal Year: 2001
    ..These experiments will thus reveal basic mechanisms responsible for epileptiform activity and thus provide a better conceptual framework for investigating human epilepsy, and for developing pharmacological treatments. ..
  54. AC6 as therapy for primary pulmonary hypertension
    Hemal Patel; Fiscal Year: 2004
    ..Understanding this higher order organization may help define new approaches to achieve the desired therapeutic end point of reduced vascular tone through viral mediated delivery of effector genes such as AC6. ..
  55. Role of Rpf Homologues in M tuberculosis Reactivation
    JoAnn Tufariello; Fiscal Year: 2004
    ....
  56. LOCAL AND LONG RANGE INTERACTIONS IN PROTEIN FOLDING
    J Scholtz; Fiscal Year: 2004
    ..abstract_text> ..
  57. Myocardial Protection in the Aging Heart
    DAVID STOWE; Fiscal Year: 2003
    ..The long term objectives of this project, as a new research area for this laboratory, are to investigate new interventions which may protect the aged myocardium from ischemia/reperfusion injury. ..
  58. HEART IMAGING AGENTS--STRUCTURAL MECHANISTICS STUDY
    David Raffel; Fiscal Year: 2001
    ..Finally, [11C]- and [18F]-labeled polar derivatives of the psychostimulant methcathinone will be synthesized as potential NET markers and their in vitro NET affinities determined as the cloned human NET transporter. ..
  59. Oxidative Stress and the Pathogenesis of Sarcopenia and Disability in Older Women
    Richard Semba; Fiscal Year: 2008
    ..AGEs are a potentially modifiable risk factor, as circulating AGEs can be lowered by dietary modification and by pharmacological intervention. ..
  60. VITAMIN A SUPPLEMENTATION FOR HIV INFECTED CHILDREN
    Richard Semba; Fiscal Year: 2002
    ....
  61. LUNG FUNCTION IN PROLONGED HEART FAILURE
    Marie Francoise Doursout; Fiscal Year: 2004
    ..After 7 days, the lungs will be analyzed to determine if connective tissue content and lung fluid have increased. These studies will test a previously unknown mechanism for the pulmonary edema associated with heart failure. ..
  62. New Target For Stroke: Peroxisome Proliferator Activated Receptor-Gamma
    Jaroslaw Aronowski; Fiscal Year: 2008
    ..3. To evaluate optimal conditions (selection of drug, dose, time window for effective treatment, tolerance, and effectiveness in permanent vs. reversible ischemia) for the anti-ischemic activity of PPARy agonists. ..