tritium

Summary

Top Publications

  1. ncbi Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine
    Pierre J Mallorga
    Merck and Co Inc, Department of Neuroscience, West Point, WP26A 3000, P O Box 4, West Point, PA 19486, USA
    Neuropharmacology 45:585-93. 2003
  2. ncbi Systematic review of experimental studies on the relative biological effectiveness of tritium
    M P Little
    Department of Epidemiology and Public Health, Imperial College, London W2 1PG, UK
    Radiat Environ Biophys 47:71-93. 2008
  3. ncbi Meal fatty acid uptake in visceral fat in women
    Susanne B Votruba
    Mayo Clinic, Endocrine Research Unit, 200 1st St SW, Rm 5 194 Joseph, Rochester, MN 55905, USA
    Diabetes 56:2589-97. 2007
  4. ncbi The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons
    A Szallasi
    National Cancer Institute, Bethesda, Maryland, USA
    Mol Pharmacol 56:581-7. 1999
  5. ncbi DNA cytosine C5 methyltransferase Dnmt1: catalysis-dependent release of allosteric inhibition
    Zeljko M Svedruzić
    Department of Chemistry and Biochemistry, University of California, Santa Barbara, California 93106, USA
    Biochemistry 44:9472-85. 2005
  6. ncbi [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Eur J Pharmacol 525:8-17. 2005
  7. ncbi Are the risks from tritium exposures being underestimated?
    F Paquet
    Institut de Radioprotection et de Surete Nucleaire, Scientific Division, BP3 13115 Saint Paul lez Durance Cedex, France
    J Radiol Prot 29:175-81. 2009
  8. pmc Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains
    Quinton L Fivelman
    Third Floor ITD, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom
    Antimicrob Agents Chemother 51:2265-7. 2007
  9. ncbi Iontophoretic estradiol skin delivery and tritium exchange in ultradeformable liposomes
    Ebtessam A Essa
    Drug Delivery Group, School of Pharmacy, University of Bradford, BD7 1DP, Bradford, UK
    Int J Pharm 240:55-66. 2002
  10. pmc In situ spatial organization of Potato virus A coat protein subunits as assessed by tritium bombardment
    L A Baratova
    N. Belozersky Institute of Physico-Chemical Biology, Moscow State University, Moscow 119899, Russia
    J Virol 75:9696-702. 2001

Detail Information

Publications244 found, 100 shown here

  1. ncbi Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine
    Pierre J Mallorga
    Merck and Co Inc, Department of Neuroscience, West Point, WP26A 3000, P O Box 4, West Point, PA 19486, USA
    Neuropharmacology 45:585-93. 2003
    ..Overall, this work shows that [3H]NFPS is a valuable tool in studying GlyT1 expression and pharmacology and that NFPS interacts with GlyT1 at a site different from the transporter translocation and ion binding sites...
  2. ncbi Systematic review of experimental studies on the relative biological effectiveness of tritium
    M P Little
    Department of Epidemiology and Public Health, Imperial College, London W2 1PG, UK
    Radiat Environ Biophys 47:71-93. 2008
    b>Tritium ((3)H) is a radioactive isotope of hydrogen. A number of factors combine to create a good deal of interest in tritium doses, both to workers and to members of the public...
  3. ncbi Meal fatty acid uptake in visceral fat in women
    Susanne B Votruba
    Mayo Clinic, Endocrine Research Unit, 200 1st St SW, Rm 5 194 Joseph, Rochester, MN 55905, USA
    Diabetes 56:2589-97. 2007
    ..Differential meal fat uptake into adipose tissue depots may be a determinant of body fat distribution...
  4. ncbi The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons
    A Szallasi
    National Cancer Institute, Bethesda, Maryland, USA
    Mol Pharmacol 56:581-7. 1999
    ..We conclude that VR1 can account for both the ligand binding and calcium uptake observed in rat DRG neurons...
  5. ncbi DNA cytosine C5 methyltransferase Dnmt1: catalysis-dependent release of allosteric inhibition
    Zeljko M Svedruzić
    Department of Chemistry and Biochemistry, University of California, Santa Barbara, California 93106, USA
    Biochemistry 44:9472-85. 2005
    ..We describe limitations in the Michaelis-Menten kinetic analysis of Dnmt1 and suggest alternative approaches...
  6. ncbi [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Eur J Pharmacol 525:8-17. 2005
    ..RHM-2), two conformationally flexible benzamide analogues, were radiolabeled with tritium (specific activity=80 Ci/mmol) and the binding of [3H]RHM-1 and [3H]RHM-2 to sigma-2 (sigma2) receptors was ..
  7. ncbi Are the risks from tritium exposures being underestimated?
    F Paquet
    Institut de Radioprotection et de Surete Nucleaire, Scientific Division, BP3 13115 Saint Paul lez Durance Cedex, France
    J Radiol Prot 29:175-81. 2009
    b>Tritium is a radionuclide that will be used and produced in fusion reactors...
  8. pmc Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains
    Quinton L Fivelman
    Third Floor ITD, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom
    Antimicrob Agents Chemother 51:2265-7. 2007
    ..Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed...
  9. ncbi Iontophoretic estradiol skin delivery and tritium exchange in ultradeformable liposomes
    Ebtessam A Essa
    Drug Delivery Group, School of Pharmacy, University of Bradford, BD7 1DP, Bradford, UK
    Int J Pharm 240:55-66. 2002
    ..Effects of current density and application time on tritium exchange with water were also determined. Penetration studies used three Protocols...
  10. pmc In situ spatial organization of Potato virus A coat protein subunits as assessed by tritium bombardment
    L A Baratova
    N. Belozersky Institute of Physico-Chemical Biology, Moscow State University, Moscow 119899, Russia
    J Virol 75:9696-702. 2001
    Potato virus A (PVA) particles were bombarded with thermally activated tritium atoms, and the intramolecular distribution of the label in the amino acids of the coat protein was determined to assess their in situ steric accessibility...
  11. ncbi Cocaine induction of dopamine transporter trafficking to the plasma membrane
    Karley Y Little
    Department of Psychiatry, University of Michigan, Ann Arbor, Michigan, USA
    Mol Pharmacol 61:436-45. 2002
    ..The present model system may further our understanding of regulatory alterations in DAT radioligand binding and function caused by cocaine exposure...
  12. ncbi Excretion and binding of tritium-labelled oestradiol in mice (Mus musculus): implications for the Bruce effect
    Adam C Guzzo
    Department of Psychology, Neuroscience and Behaviour, McMaster University, Hamilton, Ontario, Canada
    Reproduction 139:255-63. 2010
    ..When male mice were implanted with osmotic pumps containing tritium-labelled E(2) ((3)H-E(2)) or injected i.p. with (3)H-E(2), radioactivity was reliably detected in their urine...
  13. ncbi Facile and efficient postsynthetic tritium labeling method catalyzed by Pd/C in HTO
    Tomohiro Maegawa
    Laboratory of Medicinal Chemistry, Gifu Pharmaceutical University, 5 6 1, Mitahora Higashi, Gifu, 502 8585, Japan
    J Org Chem 70:10581-3. 2005
    reaction: see text] We have developed a facile and efficient tritium labeling method using a Pd/C-HTO-H2 system...
  14. ncbi Movement of a tritium plume in shallow groundwater at a legacy low-level radioactive waste disposal site in eastern Australia
    C E Hughes
    Australian Nuclear Science and Technology Organisation, Locked Bag 2001, Kirrawee DC NSW 2232, Australia
    J Environ Radioact 102:943-52. 2011
    ..Groundwater monitoring carried out since the mid 1970s indicates that with the exception of tritium, no radioactivity above typical background levels has been detected outside the immediate vicinity of the ..
  15. ncbi Systematic review of epidemiological studies of exposure to tritium
    M P Little
    Department of Epidemiology and Public Health, Imperial College, London, UK
    J Radiol Prot 28:9-32. 2008
    b>Tritium (3H) is a radioactive isotope of hydrogen. A number of factors combine to create a good deal of interest in the risks arising from exposure to tritium of both workers and members of the public...
  16. ncbi Groundwater dynamics and arsenic mobilization in Bangladesh assessed using noble gases and tritium
    Stephan Klump
    Department of Water Resources and Drinking Water, Eawag Swiss Federal Institute of Aquatic Science and Technology, Ueberlandstrasse 133, 8600 Dübendorf Switzerland
    Environ Sci Technol 40:243-50. 2006
    ....
  17. ncbi Biotic, temporal and spatial variability of tritium concentrations in transpirate samples collected in the vicinity of a near-surface low-level nuclear waste disposal site and nearby research reactor
    J R Twining
    Institute for Environmental Research, ANSTO, Locked Bag 2001, Kirrawee DC, NSW 2232, Australia
    J Environ Radioact 102:551-8. 2011
    The results of a 21 month sampling program measuring tritium in tree transpirate with respect to local sources are reported. The aim was to assess the potential of tree transpirate to indicate the presence of sub-surface seepage plumes...
  18. ncbi Body water compartment measurements: a comparison of bioelectrical impedance analysis with tritium and sodium bromide dilution techniques
    J A Simpson
    Section of Surgery, University Hospital, Queen's Medical Centre, Nottingham NG7 2UH, UK
    Clin Nutr 20:339-43. 2001
    ..using single and dual frequency bioelectrical impedance analysis (BIA) with established reference methods of tritium and NaBr dilution...
  19. ncbi Genomic methylation of peripheral blood leukocyte DNA: influences of arsenic and folate in Bangladeshi adults
    J Richard Pilsner
    Department of Environmental Health Sciences, Mailman School of Public Health, Columbia University, 60 Haven Avenue, B1, New York, NY 10032, USA
    Am J Clin Nutr 86:1179-86. 2007
    ..It is not known whether arsenic exposure influences genomic DNA methylation in human populations chronically exposed to arsenic-contaminated drinking water...
  20. ncbi Identification of a novel mitochondrial protein ("mitoNEET") cross-linked specifically by a thiazolidinedione photoprobe
    Jerry R Colca
    Pharmacia Corporation, Kalamazoo, Michigan 49001, USA
    Am J Physiol Endocrinol Metab 286:E252-60. 2004
    ..It is possible that thiazolidinedione modification of the function of the mitochondrial target may contribute to lipid lowering and/or antidiabetic actions...
  21. ncbi Femtomolar concentrations of dextromethorphan protect mesencephalic dopaminergic neurons from inflammatory damage
    Guorong Li
    Neuropharmacology Section, Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709, USA
    FASEB J 19:489-96. 2005
    ..These findings suggest a novel therapeutic concept of using "ultra-low" drug concentrations for the intervention of inflammation-related neurodegenerative diseases...
  22. ncbi Ras/ERK signalling in cannabinoid tolerance: from behaviour to cellular aspects
    Tiziana Rubino
    DBSF, Pharmacology Section, and Neuroscience Center, University of Insubria, Busto Arsizio, Italy
    J Neurochem 93:984-91. 2005
    ..These findings suggest that at least in the caudate putamen and cerebellum, the Ras/ERK pathway is essential for triggering the alteration in CB1 receptor function responsible for tolerance to THC-induced hypomotility...
  23. ncbi Measuring VLDL-triglyceride turnover in humans using ex vivo-prepared VLDL tracer
    Lars C Gormsen
    Medical Department M Endocrinology and Diabetes, Aarhus University Hospital, DK 8000 Aarhus, Denmark
    J Lipid Res 47:99-106. 2006
    ..This method for VLDL-TG tracer preparation can allow measurement of VLDL turnover, tissue uptake of VLDL-TG, and oxidation of VLDL-TG...
  24. ncbi Comparative biokinetics of tritium in rats during continuous ingestion of tritiated water and tritium-labeled food
    H Takeda
    Environmental and Toxicological Sciences Research Group, National Institute of Radiological Sciences, Japan
    Int J Radiat Biol 77:375-81. 2001
    The biokinetics of tritium during continuous ingestion of tritiated water and tritiated wheat were investigated to estimate the radiation dose rates at the end of two modes of chronic exposure.
  25. ncbi Agonist actions of "beta-blockers" provide evidence for two agonist activation sites or conformations of the human beta1-adrenoceptor
    Jillian G Baker
    Institute of Cell Signaling, Queen s Medical Centre, Nottingham NG7 2UH, UK
    Mol Pharmacol 63:1312-21. 2003
    ..The different responses to beta-blockers seen in the clinic may therefore be caused in part by these beta-blocker agonist responses and the differential activation of the two sites or conformations...
  26. pmc Selective segregation of DNA strands persists in long-label-retaining mammary cells during pregnancy
    Brian W Booth
    Mammary Biology and Tumorigenesis Laboratory, National Cancer Institute, National Institute of Health, Bethesda, MD 20892, USA
    Breast Cancer Res 10:R90. 2008
    ..Mouse mammary epithelium in nonpregnant mice contains long label-retaining epithelial cells (LREC) that divide asymmetrically and retain their template DNA strands. The role of LREC during alveogenesis has not been determined...
  27. ncbi Monte Carlo simulation of trabecular bone remodelling and absorbed dose coefficients for tritium and 14C
    R B Richardson
    Radiation Biology and Health Physics Branch, Atomic Energy of Canada Limited, Chalk River Laboratories, Chalk River, Ontario, Canada K0J 1J0
    Radiat Prot Dosimetry 127:158-62. 2007
    ..There were large differences in the absorbed fractions for two types of bone surface, quiescent and forming. Tritium in quiescent bone results in a dose to the endosteum about 20 times that for the same activity in forming bone ..
  28. ncbi Cloning and characterization of an ovine intracellular seven transmembrane receptor for progesterone that mediates calcium mobilization
    R L Ashley
    Department of Biomedical Sciences, Colorado State University, Fort Collins, Colorado 80523, USA
    Endocrinology 147:4151-9. 2006
    ..Isolation, identification, tissue distribution, cellular localization, steroid binding, and a functional response for a unique intracellular mPR in the sheep are presented...
  29. ncbi RBE and w(R) values of Auger emitters and low-range beta emitters with particular reference to tritium
    Ian Fairlie
    J Radiol Prot 27:157-68. 2007
    ..The ICRP should also publish guidance as to the methods and data sources that could be used for these RBE values...
  30. ncbi Abolition of (-)-CGP 12177-evoked cardiostimulation in double beta1/beta2-adrenoceptor knockout mice. Obligatory role of beta1-adrenoceptors for putative beta4-adrenoceptor pharmacology
    A J Kaumann
    Babraham Institute, and Department of Physiology, University of Cambridge, UK
    Naunyn Schmiedebergs Arch Pharmacol 363:87-93. 2001
    ....
  31. pmc Tritium suicide selection identifies proteins involved in the uptake and intracellular transport of sterols in Saccharomyces cerevisiae
    David P Sullivan
    Department of Biochemistry, Weill Cornell Medical College, 1300 York Ave, New York, NY 10065, USA
    Eukaryot Cell 8:161-9. 2009
    ..Upc2-1 cells were mutagenized using a transposon library, incubated with [(3)H]cholesterol, and subjected to tritium suicide selection to isolate mutants with a decreased ability to accumulate [(3)H]cholesterol...
  32. ncbi Expression of the purported sigma(1) (sigma(1)) receptor in the mammalian brain and its possible relevance in deficits induced by antagonism of the NMDA receptor complex as revealed using an antisense strategy
    K Kitaichi
    Douglas Hospital Research Centre, Department of Psychiatry, McGill University, 6875 LaSalle Blvd, Verdun, Quebec, Canada H4H 1R3
    J Chem Neuroanat 20:375-87. 2000
    ....
  33. ncbi Metabolism of paclitaxel in mice
    Heleen A Bardelmeijer
    Department of Clinical Chemistry, The Netherlands Cancer Institute Antoni van Leeuwenhoek Hospital, Amsterdam, The Netherlands
    Anticancer Drugs 14:203-9. 2003
    ..Including these metabolites, about 60% of the mass balance of paclitaxel could be quantified...
  34. ncbi Isotope dilution spaces of mice injected simultaneously with deuterium, tritium and oxygen-18
    E Krol
    Aberdeen Centre for Energy Regulation and Obesity, Department of Zoology, University of Aberdeen, Aberdeen AB24 2TZ, UK
    J Exp Biol 202:2839-49. 1999
    ..we injected 15 non-reproductive and 12 lactating mice (Mus musculus, outbred MF1) simultaneously with deuterium, tritium and oxygen-18...
  35. ncbi Effects of sex and time of day on metabolism and excretion of corticosterone in urine and feces of mice
    Chadi Touma
    Department of Behavioral Biology, Institute of Neuro and Behavioral Biology, University of Muenster, Badestrasse 9, D 48149 Muenster, Germany
    Gen Comp Endocrinol 130:267-78. 2003
    ..Since mice are extensively used in research world-wide, this could open new perspectives in various fields from ecology to behavioral endocrinology...
  36. ncbi Binding and clearance of radioactive adrenaline and noradrenaline in sheep blood
    S M El-Bahr
    Institute of Biochemistry, Department of Natural Sciences, University of Veterinary Medicine, Veterinarplatz 1, A 1210, Vienna, Austria
    Vet Res Commun 30:423-32. 2006
    ..If this could be achieved, it would yield a valuable tool for measuring the stress experienced for a longer period...
  37. pmc Inhibition of vesicular secretion in both neuronal and nonneuronal cells by a retargeted endopeptidase derivative of Clostridium botulinum neurotoxin type A
    J A Chaddock
    Centre for Applied Microbiology and Research, Porton Down, Salisbury, Wiltshire SP4 0JG, United Kingdom
    Infect Immun 68:2587-93. 2000
    ..These observations lead to the conclusion that a clostridial endopeptidase conjugate that can be used to investigate SNARE-mediated processes in a variety of cells has been successfully generated...
  38. ncbi Perirhinal and parahippocampal cortices of the macaque monkey: projections to the neocortex
    Pierre Lavenex
    Department of Psychiatry, Center for Neuroscience and California Regional Primate Research Center, UC Davis, Davis, California 95616, USA
    J Comp Neurol 447:394-420. 2002
    ..In all areas receiving heavy projections, the projections extend throughout most cortical layers, largely avoiding layer IV. We discuss these findings in relation to current theories of memory consolidation...
  39. ncbi Serotonin transporter distribution and density in the cerebral cortex of alcoholic and nonalcoholic comparison subjects: a whole-hemisphere autoradiography study
    Tuija Mantere
    Department of Forensic Psychiatry, Niuvanniemi Hospital, Kuopio, Finland
    Am J Psychiatry 159:599-606. 2002
    ....
  40. ncbi Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques
    Koppara Samuel
    Department of Drug Metabolism Merck Research Laboratories, PO Box 2000, Rahway, New Jersey 07065, USA
    J Mass Spectrom 38:211-21. 2003
    ..by reductions in the irreversible binding of radioactivity to liver microsomal material upon incubation of tritium-labeled compounds with this in vitro system...
  41. ncbi Cocaine increases dopamine uptake and cell surface expression of dopamine transporters
    Lynette C Daws
    Department of Pharmacology, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, MC 7764, San Antonio, Texas 78229 3900, USA
    Biochem Biophys Res Commun 290:1545-50. 2002
    ..Cocaine-induced increases in cell surface expression of DAT and associated changes in DA clearance represent a novel mechanism that may play a role in its addictive properties...
  42. ncbi Macaque monkey retrosplenial cortex: III. Cortical efferents
    Yasushi Kobayashi
    Department of Anatomy and Neurobiology, National Defense Medical College, Tokorozawa, Saitama 359 8513, Japan
    J Comp Neurol 502:810-33. 2007
    ....
  43. ncbi Mitogen-activated protein kinase regulates dopamine transporter surface expression and dopamine transport capacity
    Jose A Morón
    Behavioral Neuroscience Branch, National Institute on Drug Abuse, Intramural Research Program, Baltimore, Maryland 21224, USA
    J Neurosci 23:8480-8. 2003
    ..Furthermore, they highlight the potential role of MAPK as a presynaptic mechanism that regulates DA signaling...
  44. ncbi VLDL-TG kinetics: a dual isotope study for quantifying VLDL-TG pool size, production rates, and fractional oxidation in humans
    Lars P Sørensen
    Medical Department M, Aarhus University Hospital, Aarhus, Denmark
    Am J Physiol Endocrinol Metab 297:E1324-30. 2009
    ..VLDL-TG volume of distribution is therefore greater than previously anticipated. Finally our data supports that VLDL-TG contributes quantitatively to REE...
  45. ncbi Measurement of corticosterone metabolites in chicken droppings
    S Rettenbacher
    Institute of Biochemistry, University of Veterinary Medicine, Vienna, Austria
    Br Poult Sci 45:704-11. 2004
    ....
  46. ncbi Effect of nitric oxide donors on membrane tritium accumulation of endocannabinoids and related endogenous lipids
    Lina Thors
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    Eur J Pharmacol 621:10-8. 2009
    ..Here, we report that nitric oxide (NO) donors significantly increase the amount of tritium accumulated in the cell membranes of RBL2H3 rat basophilic cells, 3T3-L1 mouse fibroblast cells and b...
  47. ncbi Tritium planigraphy study of structural alterations in the coat protein of Potato virus X induced by binding of its triple gene block 1 protein to virions
    Elena Lukashina
    A N Belozersky Institute of Physico Chemical Biology, Moscow State University, Russia
    FEBS J 276:7006-15. 2009
    ..the first gene of PVX triple gene block (triple gene block 1 protein, TGBp1), to the virions were studied using tritium planigraphy...
  48. ncbi Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist
    Max Keller
    Department of Pharmaceutical Medicinal Chemistry II, Faculty of Chemistry and Pharmacy, University of Regensburg, D 93053 Regensburg, Germany
    J Med Chem 51:8168-72. 2008
    ..3)H]-UR-MK114), an easily accessible tritium-labeled NPY Y(1) receptor (Y(1)R) antagonist (K(B): 0...
  49. ncbi Basal forebrain cholinergic immunolesion by 192IgG-saporin: evidence for a presynaptic location of subpopulations of alpha 2- and beta-adrenergic as well as 5-HT2A receptors on cortical cholinergic terminals
    M Heider
    Paul Flechsig Institute for Brain Research, University Leipzig, Germany
    Neurochem Res 22:957-66. 1997
    ..The lesion-induced receptor changes suggest that the alterations in cortical 5-HT2 receptor binding observed in patients with Alzheimer's disease might be secondary to cholinergic deficits...
  50. ncbi Mechanisms of uptake and resistance to troxacitabine, a novel deoxycytidine nucleoside analogue, in human leukemic and solid tumor cell lines
    H Gourdeau
    Shire BioChem Inc, Laval, Quebec, H7V 4A7 Canada
    Cancer Res 61:7217-24. 2001
    ....
  51. ncbi Acrylamide inhibits dopamine uptake in rat striatal synaptic vesicles
    Richard M LoPachin
    Department of Anesthesiology, Albert Einstein College of Medicine, Montefiore Medical Center, Bronx, New York 10467, USA
    Toxicol Sci 89:224-34. 2006
    ..The resulting disruption of neurotransmitter storage might mediate defective presynaptic release...
  52. ncbi Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters
    Keiko Shimamoto
    Suntory Institute for Bioorganic Research, 1 1 1, Wakayamadai, Mishima gun, Osaka 618 8503, USA
    Mol Pharmacol 71:294-302. 2007
    ..The rank order of inhibition by these compounds was consistent with glutamate uptake assay results reported previously. Thus, the [3H]ETB-TBOA binding assay will be useful to screen novel EAAT ligands for all EAAT subtypes...
  53. pmc A specific membrane binding protein for progesterone in rat brain: sex differences and induction by estrogen
    S A Tischkau
    Department of Physiology and Biophysics, University of Illinois, Urbana Champaign 61801
    Proc Natl Acad Sci U S A 90:1285-9. 1993
    ..These results show a reversible sex difference in the specific binding of progesterone to synaptosomal membrane sites in the central nervous system of male and female rats which is dependent on estrogen...
  54. ncbi Interaction between a hydroxypiperidine analogue of 4-(2-benzhydryloxy-ethyl)-1-(4-fluorobenzyl)piperidine and Aspartate 68 in the human dopamine transporter
    Juan Zhen
    Department of Biological Sciences, Illinois State University, Normal, IL 61790, USA
    Eur J Pharmacol 506:17-26. 2004
    ..The present results, combined with behavioral data, implicate D68 in the dopamine transporter in cocaine antagonist activity of (+)-R,R-D-84...
  55. ncbi Effect of chronic gestational treatment with caffeine or theophylline on Group I metabotropic glutamate receptors in maternal and fetal brain
    D Leon
    Departamento de Quimica Inorganica, Organica y Bioquimica, Facultad de Quimicas, Centro Regional de Investigaciones Biomédicas, Universidad de Castilla La Mancha, Ciudad Real, Spain
    J Neurochem 94:440-51. 2005
    ..These results suggest that chronic caffeine or theophylline treatment down-regulates several mGluR/PLC transduction pathway components in both maternal and fetal brain, causing a loss of receptor responsiveness only in maternal brain...
  56. ncbi Chronic nicotine treatment attenuates alpha 7 nicotinic receptor deficits following traumatic brain injury
    S L Verbois
    Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA
    Neuropharmacology 44:224-33. 2003
    ..If TBI-induced deficits in alpha 7* nAChr expression play a role in post-injury cognitive impairment, pharmacological treatments which restore nAChr binding to control levels may be therapeutically useful...
  57. ncbi Spatial memory in aged rats is related to PKCgamma-dependent G-protein coupling of the M1 receptor
    M A Rossi
    Department of Neurological Sciences, Rush University Medical Center, Suite 334 Murdoch Building, 1653 West Congress Parkway, Chicago, IL 60612, USA
    Neurobiol Aging 26:53-68. 2005
    ..These relationships did not hold for the amygdala. Thus, individual differences in a naturally occurring age-dependent disruption of cholinergic-PKCgamma signal transduction is associated with spatial memory dysfunction...
  58. ncbi Blockade of nicotine-induced locomotor sensitization by a novel neurotensin analog in rats
    Paul Fredrickson
    Nicotine Dependence Center, Mayo Foundation for Medical Education and Research, and Mayo Clinic Jacksonville, 4500 San Pablo Road, Jacksonville, FL 32224, USA
    Eur J Pharmacol 458:111-8. 2003
    ....
  59. ncbi Melatonin exerts its analgesic actions not by binding to opioid receptor subtypes but by increasing the release of beta-endorphin an endogenous opioid
    Shaik Shavali
    Department of Pathology, University of North Dakota School of Medicine and Health Sciences, Grand Forks, ND 58203, USA
    Brain Res Bull 64:471-9. 2005
    ..Hence, it is suggested that melatonin exerts its analgesic actions not by binding to opioid receptor subtypes but by binding to its own receptors and increasing the release of beta-endorphin...
  60. pmc Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives
    Zhan Guo Gao
    Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892 0810, USA
    Mol Pharmacol 62:81-9. 2002
    ..Thus, we have identified a novel structural lead for developing allosteric enhancers of A3 adenosine receptors; such enhancers may be useful for treating brain ischemia and other hypoxic conditions...
  61. ncbi 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist
    Masaki Nakane
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Neuropharmacology 49:112-21. 2005
    ..A-381393 inhibited penile erection induced by the selective D4 agonist PD168077 in conscious rats. Thus, A-381393 is a novel selective D4 antagonist that will enhance the ability to study dopamine D4 receptors both in vitro and in vivo...
  62. ncbi Prenatal stress influences 8-OH-DPAT modulated startle responding and [3H]-8-OH-DPAT binding in rats
    W C Griffin
    Department of Neurobiology and Anatomy, Robert C Byrd Health Sciences Center, West Virginia University, Morgantown, WV 26506, USA
    Pharmacol Biochem Behav 81:601-7. 2005
    ....
  63. ncbi Derivatives of 4,6-diamino-1,2-dihydro-2-phenyl-1,2,4-triazolo[4,3-a]quinoxalin-2H-1-one: potential antagonist ligands for imaging the A2A adenosine receptor by positron emission tomography (PET)
    Marcus H Holschbach
    Institut für Nuklearchemie, Forschungszentrum Julich GmbH, D 52425 Julich, Germany
    Eur J Med Chem 40:421-37. 2005
    ..Autoradiography employing [3H]10a, showing that high unspecific binding obscured specific binding to both the A1AR and A(2A)AR. Thus, compounds 10b-s are unsuitable as ligands for imaging brain A(2A)ARs by PET...
  64. ncbi Dopamine D2 receptor stimulation of mitogen-activated protein kinases mediated by cell type-dependent transactivation of receptor tyrosine kinases
    Chunhe Wang
    Department of Behavioral Neuroscience, Oregon Health and Science University, Portland, 97239, USA
    J Neurochem 93:899-909. 2005
    ....
  65. ncbi Effects of (+/-)-huprine Y and (+/-)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors
    M M Alcalá
    Dpt de Farmacologia, de Terapeutica i de Toxicologia, Facultat de Medicina Universitat Autònoma de Barcelona, 08193 Bellaterra Barcelona, Spain
    Neurosci Lett 379:106-9. 2005
    ....
  66. ncbi Lu 28-179 labels a sigma(2)-site in rat and human brain
    Karina Krøyer Søby
    Department of Molecular Pharmacology, H Lundbeck A S, Biological Research, DK 2500, Valby, Denmark
    Neuropharmacology 43:95-100. 2002
    ..Overall, these data are consistent with [(3)H]Lu 28-179 labelling a sigma(2)-like binding site...
  67. ncbi Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503
    Sharon Rosenzweig-Lipson
    Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
    Brain Res 1073:240-51. 2006
    ....
  68. ncbi Effects of chronic dermal exposure to nonlethal doses of methyl parathion on brain regional acetylcholinesterase and muscarinic cholinergic receptors in female rats
    Tangeng Ma
    Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson, Mississippi 39216, USA
    J Neurosci Res 71:138-45. 2003
    ..Because central respiratory neurons gather in the brain stem, preferential effects there and in other brain regions may underlie lethal toxicity of methyl parathion and other organophosphates...
  69. ncbi Quantitative in vitro phosphor imaging using [3H] and [18F] radioligands: the effects of chronic desipramine treatment on serotonin 5-HT2 receptors
    Elissa M Strome
    Pacific Parkinson s Research Centre and UBC TRIUMF PET Group, University of British Columbia, Purdy Pavilion M36, 2221 Wesbrook Mall, Vancouver, B C, Canada V6T 2B5
    J Neurosci Methods 141:143-54. 2005
    ..We also present data on the reusability of tritium-sensitive phosphor screens, and show that the use of simple corrections allows receptor binding data with PET ..
  70. ncbi Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic administration
    Marzena Karcz-Kubicha
    Preclinical Pharmacology Section, Behavioral Neuroscience Branch, NIDA, NIH, IRP, Department of Health and Human Services, Baltimore, MD, USA
    Neuropsychopharmacology 28:1281-91. 2003
    ....
  71. ncbi Molecular mechanisms involved in the asymmetric interaction between cannabinoid and opioid systems
    Daniela Vigano
    DBSF, Pharmacology Section and Neuroscience Center, University of Insubria, Via A da Giussano 10, 21052, Busto Arsizio, VA, Italy
    Psychopharmacology (Berl) 182:527-36. 2005
    ..This might open up new therapeutic opportunities for relief of chronic pain through cannabinoid-opioid coadministration...
  72. ncbi The inhibitory role of methylation on the binding characteristics of dopamine receptors and transporter
    Eun Sook Y Lee
    College of Pharmacy and Pharmaceutical Sciences, Florida A and M University, Tallahassee, FL 32307, USA
    Neurosci Res 48:335-44. 2004
    ..We propose that the SAM effect might be related to its ability to react with dopamine receptor proteins through methyl-ester formation and methanol production following the hydrolysis of the carboxyl-methylated receptor proteins...
  73. ncbi Pharmacological actions of a novel and selective dopamine D3 receptor antagonist, KCH-1110
    Woo Kyu Park
    Pharmaceutical Screening Research Team, Korea Research Institute of Chemical Technology, 100 Jang Dong, Yusong gu, Daejon 305 343, South Korea
    Pharmacol Res 48:615-22. 2003
    ..The present studies, therefore, suggest that KCH-1110 is a potent and relatively selective dopamine D3 receptor antagonist with antipsychotic actions...
  74. ncbi Binding characteristics of [3H]ucb 30889 to levetiracetam binding sites in rat brain
    Michel Gillard
    UCB S A, Pharma Sector, In Vitro Pharmacology, Building R4, Chemin du Foriest, B 1420 Braine l Alleud, Belgium
    Eur J Pharmacol 478:1-9. 2003
    ..Preliminary autoradiography studies in rat brain revealed that [3H]ucb 30889 labels specific sites in all brain regions and that this binding is concentration-dependently displaced by levetiracetam...
  75. ncbi Carvedilol blockade of rat myocardial alpha1-adrenoceptors
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, P O Box 1057 Blindern, N 0316 Oslo, Norway
    Eur J Pharmacol 481:83-9. 2003
    ..Thus, carvedilol antagonizes the myocardial alpha(1)-adrenoceptors with a 9-fold lower potency than the beta-adrenoceptors. Antagonism of myocardial alpha(1)-adrenoceptor evoked effects may contribute to clinical effects of carvedilol...
  76. ncbi Antiparkinson concentrations of pramipexole and PHNO occupy dopamine D2(high) and D3(high) receptors
    Philip Seeman
    Department of Pharmacology, Medical Sciences Building, Toronto, Ontario, Canada
    Synapse 58:122-8. 2005
    ..The D3(High) receptors are less selectively occupied by +PHNO, bromocriptine, apomorphine, and -NPA...
  77. ncbi Hypotensive effects of eugenosedin-A with serotonin, alpha- and beta-adrenoceptor antagonistic activities in spontaneously hypertensive and normotensive rats
    Kuo Pyng Shen
    Department of Pharmacology, College of Medicine, Kaohsiung Medical University, Taiwan
    Pharmacology 71:91-101. 2004
    ..Finally, we suggest that the hypotensive effects of eugenosedin-A can be attributed to its multiple actions on the blockade of 5-HT1B, 5-HT2A, alpha and beta1 receptors in both WKY and SHR strains...
  78. pmc Low concentrations of neuroactive steroids alter kinetics of [3H]ifenprodil binding to the NMDA receptor in rat frontal cortex
    Tobias Johansson
    Department of Pharmaceutical Biosciences, Division of Biological Research on Drug Dependence, Uppsala University, P O Box 591, S 751 24 Uppsala, Sweden
    Br J Pharmacol 146:894-902. 2005
    ..In conclusion, the present study show that the allosteric modulators PS or 3alpha5betaS change [3H]ifenprodil binding kinetics in a way indicating conformational alteration of its binding site on the NR2B subunit...
  79. ncbi Differences in interactions with the dopamine transporter as revealed by diminishment of Na(+) gradient and membrane potential: dopamine versus other substrates
    Juan Zhen
    Department of Biological Sciences, Illinois State University, Normal, IL, USA
    Neuropharmacology 49:769-79. 2005
    ..In contrast, non-dopamine substrates may not be able to readily interact with this state from either side of the membrane...
  80. ncbi High-affinity binding of beta-carbolines to imidazoline I2B receptors and MAO-A in rat tissues: norharman blocks the effect of morphine withdrawal on DOPA/noradrenaline synthesis in the brain
    Antonio Miralles
    Laboratori de Neurofarmacologia, Institut Universitari d Investigacio en Ciencies de la Salut, Universitat de les Illes Balears, Ctra Valldemossa km 7 5, E 07122, Palma de Mallorca, Spain
    Eur J Pharmacol 518:234-42. 2005
    ..The results indicate that beta-carbolines bind with high affinity to imidazoline I2B receptors, and similarly to I2 ligands (LSL 60101) can block the behavioural and biochemical effects of opiate withdrawal...
  81. ncbi [3H]linopirdine binding to rat brain membranes is not relevant for M-channel interaction
    Christian Wolff
    Deparment of in vitro Pharmacology, UCB SA, CNS Preclinical Research, Chemin du Foriest R4, 1420 Braine L Alleud, Belgium
    Eur J Pharmacol 518:10-7. 2005
    ..The results obtained in this study demonstrate that [(3)H]linopirdine binding to rat brain and rat liver membranes is representative for CYP450 interaction and not relevant for the binding to the M-channel proteins...
  82. ncbi Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors
    Sutapa Mukherjee
    Neuroscience Disease Research, Global Pharmaceutical Research and Development, AP9A 3, Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064, USA
    Eur J Pharmacol 505:1-9. 2004
    ..The findings of the pharmacological differences between the human and rat cannabinoid CB2 receptors in this study provide critical information for characterizing cannabinoid ligands in in vivo rodent models for drug discovery purpose...
  83. ncbi Use of [3H]fluorowillardiine to study properties of AMPA receptor allosteric modulators
    Markus Kessler
    Department of Pharmacology, Southern Illinois University School of Medicine, 801 N Rutledge, PO Box 19629, Springfield, IL 62794 9629, USA
    Brain Res 1076:25-41. 2006
    ..Lastly, data are shown which highlight the importance of optimizing experimental conditions in filtration assays, for instance by always including thiocyanate in wash buffers...
  84. ncbi Quantitative autoradiographic analysis of the new radioligand [(3)H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid ([(3)H]NCS-382) at gamma-hydroxybutyric acid (GHB) binding sites in rat brain
    Georgianna G Gould
    Department of Pharmacology, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, 78229 3900, San Antonio, TX, USA
    Brain Res 979:51-6. 2003
    ..The distribution of GHB binding sites as defined by [(3)H]NCS-382 suggests that GHB may play a role in neuromodulation or neurotransmission in frontal brain areas...
  85. ncbi Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist
    Mariana Spetea
    Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Innsbruck, Innrain 52a, A 6020 Innsbruck, Austria
    Eur J Neurosci 18:290-5. 2003
    ..14-methoxymetopon (4,5alpha-epoxy-3-hydroxy-14beta-methoxy-5beta,17-dimethylmorphinan-6-one) was prepared in tritium labelled form by a catalytic dehalogenation method resulting in a specific radioactivity of 15.9 Ci/mmol...
  86. ncbi Choline is transported by vesicular acetylcholine transporter
    Dawn T Bravo
    Department of Chemistry and Biochemistry, University of California, Santa Barbara, California 93106 9510, USA
    J Neurochem 91:766-8. 2004
    ..Ch transport by VAChT is of interest in view of the possibilities that Ch (i) occurs at higher concentration than ACh does in terminal cytoplasm under some conditions, and (ii) is an agonist for alpha 7 nicotinic receptors...
  87. ncbi Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist
    Claire L Neilan
    Department of Pharmacology, University of Michigan, 1301 Medical Science Res Bldg III, Ann Arbor, MI 48109, USA
    Eur J Pharmacol 499:107-16. 2004
    ..BU72 is too efficacious for human use but manipulation to reduce efficacy could provide a lead to the development of a treatment for opioid dependence...
  88. ncbi Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist
    Richard W Ransom
    Department of Molecular Neurology, Merck Research Laboratories, WP46 300, West Point, PA 19486, USA
    Eur J Pharmacol 499:77-84. 2004
    ..The high signal-to-noise ratio obtained with [35S]compound A will allow this ligand to be a very useful tool for future investigations of the bradykinin B1 receptor...
  89. ncbi Increased phencyclidine-induced hyperactivity following cortical cholinergic denervation
    Anna Mattsson
    Department of Neuroscience, Retzius Laboratory, Karolinska Institute, Stockholm, Sweden
    Neuroreport 16:1815-9. 2005
    ..These results suggest that aberrations in cholinergic function might lead to glutamatergic dysfunctions, which might be of relevance for the pathophysiology for schizophrenia...
  90. ncbi Binding of [3H]mazindol to cardiac norepinephrine transporters: kinetic and equilibrium studies
    David M Raffel
    Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, 3480 Kresge III Building, Ann Arbor 48109 0552, USA
    Naunyn Schmiedebergs Arch Pharmacol 370:9-16. 2004
    ..These studies demonstrate the high selectivity of [3H]mazindol binding for the norepinephrine transporter in membrane preparations from mammalian hearts...
  91. ncbi Antidepressant drug induced alterations in binding to central dopamine transporter sites in the Wistar Kyoto rat strain
    Xilu Jiao
    University of the Sciences in Philadelphia, Department of Pharmacology and Toxicology Box 118, 600 South 43rd Street, Philadelphia, PA 19104, USA
    Prog Neuropsychopharmacol Biol Psychiatry 30:30-41. 2006
    ....
  92. pmc Methylmercury elicits rapid inhibition of cell proliferation in the developing brain and decreases cell cycle regulator, cyclin E
    Kelly Burke
    Department of Neuroscience and Cell Biology, UMDNJ Robert Wood Johnson Medical School, Piscataway, NJ 08854, USA
    Neurotoxicology 27:970-81. 2006
    ..In aggregate, our observations identify the G1/S transition as an early target of MeHg toxicity and raise the possibility that cyclin E degradation contributes to both decreased proliferation and eventual cell death...
  93. pmc Regional localization and developmental profile of acetylcholinesterase-evoked increases in [(3)H]-5-fluororwillardiine binding to AMPA receptors in rat brain
    S Olivera
    MRC Centre for Synaptic Plasticity, Anatomy Department, School of Medical Sciences, University of Bristol, University Walk, Bristol, BS8 1TD, UK
    Br J Pharmacol 133:1055-62. 2001
    ..These findings suggest that modulation of AMPA receptors could provide one molecular mechanism for the previously reported effects of AChE on synapse formation, synaptic plasticity and neurodegeneration...
  94. pmc Low concentrations of ethanol do not affect radioligand binding to the delta-subunit-containing GABAA receptors in the rat brain
    Ashok K Mehta
    Department of Pharmacology, MC 7764, The University of Texas Health Science Center, 7703 Floyd Curl Drive, San Antonio, TX 78229 3900, USA
    Brain Res 1165:15-20. 2007
    ..These results suggest that the native delta-subunit-containing GABA(A) receptors do not play a major role in the pharmacology of clinically relevant low concentrations of ethanol...
  95. ncbi Characterization of cannabinoid-binding sites in zebrafish brain
    Ivan Rodriguez-Martin
    Department of Biochemistry and Molecular Biology, Faculty of Medicine, Instituto de Neurociencias de Castilla y Leon, University of Salamanca, Spain
    Neurosci Lett 413:249-54. 2007
    ..Hence the study of zebrafish cannabinoid activity may contribute to an understanding of the endogenous cannabinoid system in higher vertebrates...
  96. ncbi Clusterin enhances proliferation of primary astrocytes through extracellular signal-regulated kinase activation
    Yong Jae Shin
    Department of Pharmacology and BK21 Program for Medical Sciences, College of Medicine, Korea University, Seoul, Korea
    Neuroreport 17:1871-5. 2006
    ..These results suggest that clusterin might play an important role in astrogliosis by stimulating the proliferation of astrocytes through activation of the extracellular signal-regulated kinase 1/2 signaling pathway...
  97. ncbi Increase in A2A receptors in the nucleus accumbens after extended cocaine self-administration and its disappearance after cocaine withdrawal
    Daniel Marcellino
    Department of Neuroscience, Karolinska Institutet, 17177 Stockholm, Sweden
    Brain Res 1143:208-20. 2007
    ..A(2A) agonists may therefore represent cocaine antagonist drugs to be used in treatment of cocaine addiction acting inter alia by antagonizing signaling in accumbens A(2A)/D(2) and A(2A)/D(3) heteromers...
  98. ncbi 1-(m-chlorophenyl)piperazine (mCPP) dissociates in vivo serotonin release from long-term serotonin depletion in rat brain
    M H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Neuropsychopharmacology 24:492-501. 2001
    ..Our data support the notion that 5-HT release per se may not be sufficient to produce the long-term 5-HT deficits associated with d-fenfluramine and other amphetamines...
  99. pmc Brain alpha(2)-adrenoceptors in monoamine-depleted rats: increased receptor density, G coupling proteins, receptor turnover and receptor mRNA
    C Ribas
    Laboratory of Neuropharmacology, Associate Unit of the Institute Cajal/CSIC, Department of Biology, University of the Balearic Islands, Cra. Valldemossa Km 7.5, E-07071 Palma de Mallorca, Spain
    Br J Pharmacol 132:1467-76. 2001
    ..This transcriptional activation of the receptor gene expression appears to be the cellular mechanism by which reserpine induces up-regulation in the density of brain alpha(2)-adrenoceptors...
  100. ncbi Estrogenic activity of tamoxifen and raloxifene on rat brain AMPA receptors
    M Cyr
    Oncology and Molecular Endocrinology Research Center, Laval University Medical Center and Faculty of Pharmacy, Laval University Quebec, Sainte-Foy, Canada
    Neuroreport 12:535-9. 2001
    ..Hence, tamoxifen and raloxifene showed agonist estrogenic activity on AMPA receptors in specific brain regions, which can be dissociated from their antagonist estrogenic activity in the periphery...
  101. ncbi Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models
    Atsuyuki Kohara
    Pharmacology Laboratories, Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba 305 8585, Japan
    Eur J Pharmacol 571:8-16. 2007
    ..YM-230888 has potential as a new analgesic agent for the treatment of various chronic pain conditions. In addition, YM-230888 may be a useful tool for the investigation of mGlu(1) receptors...

Research Grants63

  1. Aging and Myocardial Progenitor Recruitment
    Richard T Lee; Fiscal Year: 2013
    ..Until recently, methods for tracking cell division relied mainly on BrdU incorporation or tritium (3H) labeling;these techniques have limitations because they do not always have sufficient resolution to track ..
  2. Prevention of Biofilm Related Infections Using a Novel, Broad Spectrum Antimicrob
    ROY DRAKE BLOEBAUM; Fiscal Year: 2013
    ..Furthermore, a second phase of the study will use tritium as a radiolabel on CSA-13 to determine the local and systemic effects of CSA-13 on tissue...
  3. How glucose transporter structure affects its function
    Anthony Carruthers; Fiscal Year: 2013
    ..GLUT1 hydrogens (80%) undergo conformation-sensitive exchange with solvent tritium or deuterium but which amino acids exchange is unknown...
  4. Evaluation of Tritium: Relative Biological Effectiveness and Cancer Mortality
    David B Richardson; Fiscal Year: 2011
    ..Even less is understood about the effects of chronic exposure to beta-emitters, such as tritium, a low- energy radioisotope of hydrogen that is produced through nuclear fuel production...
  5. The role and mechanisms of lipofuscin formation in macular degeneration
    Ilyas Washington; Fiscal Year: 2013
    ..ocular pharmacokinetics of vitamin A and its dimers we track their fate and/or biosynthesis using deuterium or tritium labeled species...
  6. Blood Brain Barrier Dysfunction in Parkinson's Diseases
    Paul M Carvey; Fiscal Year: 2010
    ..neuron loss in mice with pre-existing DA lesions (induced b MPTP and LPS) for evidence of an increased entry of a tritium labeled, systemic By administered, DA neurotoxin (MPP+), and immune mediators...
  7. Bone-seeking proteasome inhibitors for myeloma
    Joseph Agyin; Fiscal Year: 2009
    ..PI-BP conjugates as a means of selective delivery of PS341 and MG262 to bone, ii) To synthesize C-14-and C-14/tritium-labeled PS341- and MG262-BP conjugates to study the bioavailability and homing capabilities of the conjugates in ..
  8. Characterization of Pseudouridene Synthase TruD
    CLAUDIA CAROLINA RECINOS; Fiscal Year: 2010
    ..coli TruD homolog. Using standard biochemical means, including tritium release and filter binding assays, we will examine the features of the tRNA substrate and those of the enzyme, ..
  9. Molecular Control of cGMP Signaling by PKGs and PDEs
    Jackie Corbin; Fiscal Year: 2007
    ..Three potentially commercialized PDE5 inhibitors (sildenafil, vardenafil, tadalafil) have been labeled with tritium. They will be used to identify and quantify PDE5 and PDE11 in crude tissue extracts, and to search for other PDE ..
  10. RADIOLIGANDS FOR CENTRAL NORADRENERGIC UPTAKE SITES
    Shanaz Tejani Butt; Fiscal Year: 1992
    ..Potential ligands will be radiolabelled with tritium to high specific activity and their binding properties will be investigated both in vitro and in vivo...
  11. An Epithermal Neutron Source for Cancer Therapy
    MELVIN PIESTRUP; Fiscal Year: 2006
    ..b>Tritium storage, replenishing and recycling will be achieved by a self-contained vacuum system to minimize radiation and ..
  12. MECHANISMS OF DRUG DEPOSITION IN HAIR
    JAMES RUTH; Fiscal Year: 2002
    ..Accessible water space was determined using a stage micrometer and equilibration of hairs with tritium oxide of known specific activity; (2) serum constituents as [C-14]urea, [Ca-45]calcium+2, [Cl-36]chloride- were ..
  13. Damage signaling from irradiated to non-irradiated cells
    EDOUARD AZZAM; Fiscal Year: 2004
    ..2) Bystander cells mixed with cells radiolabeled with the short-range beta-particle emitter tritium and seeded in sufficient numbers to achieve confluent monolayers...
  14. ROLE OF PEPTIDOGLYCAN IN HEALTH AND DISEASE
    RAOUL ROSENTHAL; Fiscal Year: 1993
    ..by fast-atom bombardment-mass spectrometry and, for some purposes, labeled to very high specific activity with tritium. In conjunction with assay systems for quantitating the release of soluble PG by cultured bacteria and for ..
  15. CHARACTERIZATION OF PRONASE ENZYMES
    WILLIAM AWAD; Fiscal Year: 1980
    ..The studies on guanidinated proteins will be extended so that exchange-in studies with tritium will be complemented by exchange-out studies...
  16. BMP-2 Releasing Implant Surface for Bone Regeneration
    RAJIV SATSANGI; Fiscal Year: 2003
    ..A radioactive version of the surface modification will also be made, using tritium labeled linker and the release of the protein over time will be measured conveniently...
  17. RESPIRATORY NEURONS: NEUROCHEMICAL INTERRELATIONSHIPS
    Madhu Kalia; Fiscal Year: 1991
    ..The application of two different neuroanatomical labels, tritium labeled horseradish peroxidase and cholera toxin conjugated with horseradish peroxidase, in combination with ..
  18. SQUALENE AND OXIDOSQUALENE CYCLASES
    Glenn Prestwich; Fiscal Year: 2002
    ..There are six specific goals. First, unlabeled and tritium-labeled analogs, inhibitors and photoaffinity labels will be synthesized and assayed as mechanistic probes...
  19. HOW DO ENZYMES GENERATE AND CONTROL FREE RADICALS
    E Marsh; Fiscal Year: 1999
    ..Tritiated substrates and coenzyme will be used in stopped-flow experiments to measure the rates of tritium transfer between substrate, coenzyme and product in both directions...
  20. MECHANISMS OF CHAIN ELONGATION OF ALPHA-KETO ACIDS
    Carl Stevens; Fiscal Year: 1980
    ..Tests of proton migration in the isomerization step involve the synthesis of substrates labeled with tritium at specific sites...
  21. SMALL MOLECULE ORPHANIN FQ/NOCICEPTIN RECEPTOR LIGANDS
    Richard Houghten; Fiscal Year: 2000
    ..Using a tritium labeled form of this peptide, a radioreceptor binding assay has been developed using rat brain homogenates...
  22. MINORITY PREDOCTORAL FELLOWSHIP PROGRAM
    NATASHA NESBITT; Fiscal Year: 2005
    ..This will be carried out by determining whether AdoMet binds to LAS and by assessing whether tritium or deuterium is transferred to 5'- deoxyadenosine from various isotopically labeled forts of octanoic acid...
  23. HUMAN METABOLISM OF TAXOL
    Eric Rowinsky; Fiscal Year: 1993
    ..To accomplish these goals, tritium- and deuterium-labeled taxol will be synthesized...
  24. CHAPERONIN AIDED PROTEIN FOLDING OF RHODANESE
    PAUL HOROWITZ; Fiscal Year: 2002
    ..Fluorescence and tritium exchanges will monitor flexibility; and hydrodynamic methods will monitor size and quaternary structure...
  25. RENAL TRANSPORT AND METABOLISM OF PROTEINS
    Thomas Maack; Fiscal Year: 1992
    ..In all of these studies a new metod of labelling proteins with tritium to very high specific activity without changes in structure, antigenicity and biological activity of the ..
  26. METABOLIC STEREOISOMERIC INVERSION OF CHIRAL DRUGS
    Ching Shih Chen; Fiscal Year: 1993
    ..In the elucidation of inversion mechanism, chiral tritium-labeled 2- arylpropionic acids will be synthesized and exposed to the homogenate of the liver and other organs of ..
  27. PROTEIN BIOSYNTHESIS AS A FUNCTION OF AGE OR CANCER
    ROBERT LOFTFIELD; Fiscal Year: 1980
    Rat albumin is labeled in vivo with tritium labeled amino acids. The albumin is purified and fragmented into peptides of 6 to 30 amino acid residues by a succession of treatments such as CNBr, trypsin and chymotrypsin...
  28. STUDIES ON GLYCOGEN SYNTHESIS & GLUCONEOGENESIS
    Joseph Katz; Fiscal Year: 1993
    ..The radioactive tracer used here is water labeled with tritium (3HOH)...
  29. SOLID STATE DETECTOR FOR GAS CHROMATOGRAPHY
    MIKE SQUILLANT; Fiscal Year: 1999
    ..photodiodes (APDs), which have demonstrated the ability to detect low energy beta particles, including those from tritium, with high efficiency...
  30. PHYSICAL STUDIES OF PROTEIN INTERACTIONS
    James Lee; Fiscal Year: 1992
    ..is important in enzyme regulation, the global structural changes induced by ligands will be monitored by tritium exchange...
  31. DIABETIC RETINOPATHY: BASIC STUDY IN PERICYTE METABOLISM
    Weiye Li; Fiscal Year: 1993
    ..The incorporation of tritium-labelled thymidine, an index of cell proliferation, will be used to correlate components of the inositol ..
  32. CANNABINOID INVESTIGATIONS
    Raphael Mechoulam; Fiscal Year: 1992
    ..II. We plan to prepare two new types of cannabinoid probes (labelled with tritium on the methyl group of cyclohexene ring and on one of the methyl groups of the pyran ring)...
  33. SYNTHESIS/DISTRIBUTION OF DRUGS OF ABUSE AND OPIODS
    F Carroll; Fiscal Year: 2000
    ..Radiolabeled compounds are prepared in specific activities ranging up to 75 Ci/mmole if tritium- labeled and up to 300 Ci/mmole if iodine-125-labeled...
  34. BIOMEDICAL RESEARCH SUPPORT
    Harlyn Halvorson; Fiscal Year: 1991
    ..solid state materials, (j) in vivo 23Na NMR of insect larvae, (k) NMR of blood serum trace components, and (l) tritium NMR of high specific activity radioligands complexed to binding proteins...
  35. CULTURED LACTOTROPHS: A DOPAMINERGIC RECEPTOR MODEL
    Mark Heiman; Fiscal Year: 1980
    ..After 96 hours of culture, dopaminergic receptor characteristics will be investigated using tritium-labeled ligands such as (3H)-spiroperidol, (3H)-haloperidol and (3H)-dopamine...
  36. THE PHOTOBIOLOGY OF VITAMIN D
    Michael Holick; Fiscal Year: 2005
    ..This will be accomplished by making tritium-labeled toxisterols and sprasterols, and evaluating their metabolism in cultured human keratinocytes...
  37. Tritum AMS Analysis of Cancer Biomarkers
    Paul Skipper; Fiscal Year: 2007
    ..develop a high-throughput, ultra-sensitive accelerator mass spectrometer for the detection and quantification of tritium in labeled biological molecules...
  38. Chaperonin-mediated protein folding
    Arthur Horwich; Fiscal Year: 2007
    ..to GroEL-substrate complexes produces an active, forced, unfolding of substrate protein prior to its release into the central cavity will be studied using tritium and hydrogen/deuterium exchange experiments. [unreadable] [unreadable]
  39. NEW SEROTONIN TRANSPORTER IMAGING AGENTS BY DESIGN
    John Gerdes; Fiscal Year: 2000
    ..assessments of the ligands using rat tissues; 3) the formation of radiolabeled forms of the ligands (tritium and also carbon-11 and fluorine-18 variants); 4) evaluation of the radiotracers both in vivo and ex vivo with rat ..
  40. TRANSPORT OF LDL IN THE ARTERIAL WALL
    Clark Colton; Fiscal Year: 1992
    ..In vivo uptake experiments with radiodinated and tritium-labeled LDL will be analyzed with quantitative autoradiography...
  41. TRITIUM LABELING-MECHANISMS AND METHODS
    CHIN TZU PENG; Fiscal Year: 1992
    The objective of the proposed research is to study the conditions under which tritium labeled compounds such as unsaturates, polypeptides, proteins, and biomolecules, can be obtained with high specific activity and minimum degradation...
  42. NON-AROMATIZING ANDROGEN 19-DESMOLASE AND 19-HYDROXYLASE
    Yoshio Osawa; Fiscal Year: 1990
    ..The methods involve synthesis of steroids with and without deuterium, tritium, carbon-14 and oxygen-18 labels at stereoselective and/or regiospecific positions, structural studies and isotope ..
  43. Gene-Gene Interactions in Pulmonary Hypertension
    ELISABETH WILLERS; Fiscal Year: 2006
    ..EBV-transformed, patient lymphoblastoid cell lines to quantifiy mRNA and perform cell function assays with tritium-labeled serotonin (5-HT) and a liquid scintillation counter...
  44. PREPARATION OF RADIOLABELED ANTI-AIDS COMPOUNDS
    J Kepler; Fiscal Year: 1993
    ..the major emphasis being on the preparation of the desire labeled materials via synthetic procedure using 14C and tritium. Major emphasis will be on the preparation of the desired radiolabeled compounds via synthetic procedures and ..
  45. PREPARATION OF RADIOLABELED ANTI-AIDS COMPOUNDS
    JOHN KEPLER; Fiscal Year: 1990
    ..emphasis being on the preparation of the desired labeled materials via synthetic procedures using carbon 14 and tritium. Major emphasis will be on the preparation of the desired radiolabeled compounds via synthetic procedures and ..
  46. SEPARATION OF BIOMOLECULES BY ELECTROMATOGRAPHY
    JOSEPH PESEK; Fiscal Year: 1993
    ..The effects of residual silanols will be studied by tritium-labeling experiments...
  47. TRITIUM AMS ANALYSIS OF CANCER BIOMARKERS
    Paul Skipper; Fiscal Year: 2001
    ..Applicant's Description) The goal of this project is to develop an exceptionally compact, high throughput tritium accelerator mass spectrometer (AMS) to enable ultra-sensitive tracer studies relevant to the molecular analysis ..
  48. STEROID UPTAKE IN HORMONALLY DEPENDENT CANCERS
    George Barrows; Fiscal Year: 1980
    ..All the radiographic methods have been developed for correlation with the steroid receptor uptake, and tritium labelled compounds will be submitted to collaborators for verification of biologic activity (and absence of ..
  49. MYOINOSITOL 1,4,5-TRISPHOSPHATE RECEPTOR
    CLINTON BALLOU; Fiscal Year: 1990
    ..The demonstration of the receptor will be based on binding studies using a tritium-labeled analog of myoinositol trisphosphate, and the isolation of the receptor will make use of an immobilized ..
  50. HIGH-AFFINITY LIGANDS FOR THE COCAINE RECEPTOR
    JOHN NEUMEYER; Fiscal Year: 1991
    ..In Phase I, a tritium-labeled p-fluorophenyl cocaine analog was prepared whose higher affinity and specific activity represented a ten-..
  51. PHARMACOKINETIC & TISSUE DISTRIBUTION OF H3-EGCG
    Carol Green; Fiscal Year: 2000
    The pharmacokinetics of tritium-labeled epigallocatechin gallate will be evaluated in dogs after single, intravenous administration...
  52. Novel pharmacotherapies for treatment of ADHD
    FRANK TARAZI; Fiscal Year: 2003
    ..Expected findings should evolve new principles and lead to novel compounds that can be used as much-needed innovative treatments for ADHD and other major neuropsychiatric disorders. ..
  53. Norepinephrine Transporters: Targets for ADHD
    FRANK TARAZI; Fiscal Year: 2004
    ..Expected findings should lead to novel compounds that can be developed as much needed innovative non-stimulant treatments for ADHD and other major neuropsychiatric disorders. ..
  54. Effects of antipsychotic drugs on brain and behavior
    FRANK TARAZI; Fiscal Year: 2005
    ..adult rats, and should evolve new principles for improved treatments for childhood-onset schizophrenia and other major pediatric psychiatric disorders. ..
  55. New PET Radiotracers-Monoamine Transporters
    Michael Kilbourn; Fiscal Year: 2003
    ....
  56. Hybrid Drugs: Novel Pharmacotherapy for ADHD
    FRANK TARAZI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  57. Animal Models of Childhood and Adolescent Depression
    David Bylund; Fiscal Year: 2005
    ..abstract_text> ..
  58. Adrenergic Receptors During Periadolescent Development
    David Bylund; Fiscal Year: 2005
    ..abstract_text> ..
  59. C elegans:a model to study intestinal water-soluble vitamins transport in vivo
    HAMID SAID; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  60. The Influence of Static Magnetic Fields on Brain tissue
    Andrzej Wieraszko; Fiscal Year: 2003
    ..The cell excitability, synaptic efficiency and action potentials recorded from the slices exposed to SMF will be studied. The directions of alternative and future research are delineated. ..
  61. ESTROGEN EFFECTS ON DOPAMINE AUTORECEPTOR ACTIVITY
    Tina Thompson; Fiscal Year: 2003
    ....