- 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...
- 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...
- 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...
- The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons
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...
- 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...
- [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe
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 ..
- Are the risks from tritium exposures being underestimated?
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...
- 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...
- 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...
- 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...
- 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...
- 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...
- Facile and efficient postsynthetic tritium labeling method catalyzed by Pd/C in HTO
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...
- 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 ..
- 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...
- Groundwater dynamics and arsenic mobilization in Bangladesh assessed using noble gases and tritium
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
- 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...
- 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...
- 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...
- 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...
- Femtomolar concentrations of dextromethorphan protect mesencephalic dopaminergic neurons from inflammatory damage
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...
- Ras/ERK signalling in cannabinoid tolerance: from behaviour to cellular aspects
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...
- 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...
- Comparative biokinetics of tritium in rats during continuous ingestion of tritiated water and tritium-labeled food
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.
- 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...
- 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...
- 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 ..
- 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...
- RBE and w(R) values of Auger emitters and low-range beta emitters with particular reference to tritium
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...
- 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
- 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...
- 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
Douglas Hospital Research Centre, Department of Psychiatry, McGill University, 6875 LaSalle Blvd, Verdun, Quebec, Canada H4H 1R3
J Chem Neuroanat 20:375-87. 2000
- 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...
- Isotope dilution spaces of mice injected simultaneously with deuterium, tritium and oxygen-18
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...
- Effects of sex and time of day on metabolism and excretion of corticosterone in urine and feces of mice
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...
- 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...
- 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...
- Perirhinal and parahippocampal cortices of the macaque monkey: projections to the neocortex
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...
- Serotonin transporter distribution and density in the cerebral cortex of alcoholic and nonalcoholic comparison subjects: a whole-hemisphere autoradiography study
Department of Forensic Psychiatry, Niuvanniemi Hospital, Kuopio, Finland
Am J Psychiatry 159:599-606. 2002
- Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques
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...
- 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...
- Macaque monkey retrosplenial cortex: III. Cortical efferents
Department of Anatomy and Neurobiology, National Defense Medical College, Tokorozawa, Saitama 359 8513, Japan
J Comp Neurol 502:810-33. 2007
- 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...
- 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...
- Measurement of corticosterone metabolites in chicken droppings
Institute of Biochemistry, University of Veterinary Medicine, Vienna, Austria
Br Poult Sci 45:704-11. 2004
- Effect of nitric oxide donors on membrane tritium accumulation of endocannabinoids and related endogenous lipids
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...
- 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
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...
- 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
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...
- 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
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...
- Mechanisms of uptake and resistance to troxacitabine, a novel deoxycytidine nucleoside analogue, in human leukemic and solid tumor cell lines
Shire BioChem Inc, Laval, Quebec, H7V 4A7 Canada
Cancer Res 61:7217-24. 2001
- 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...
- Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters
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...
- 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...
- Interaction between a hydroxypiperidine analogue of 4-(2-benzhydryloxy-ethyl)-1-(4-fluorobenzyl)piperidine and Aspartate 68 in the human dopamine transporter
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...
- Effect of chronic gestational treatment with caffeine or theophylline on Group I metabotropic glutamate receptors in maternal and fetal brain
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...
- 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...
- 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...
- Blockade of nicotine-induced locomotor sensitization by a novel neurotensin analog in rats
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
- Melatonin exerts its analgesic actions not by binding to opioid receptor subtypes but by increasing the release of beta-endorphin an endogenous opioid
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...
- 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...
- 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist
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...
- 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
- 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...
- Dopamine D2 receptor stimulation of mitogen-activated protein kinases mediated by cell type-dependent transactivation of receptor tyrosine kinases
Department of Behavioral Neuroscience, Oregon Health and Science University, Portland, 97239, USA
J Neurochem 93:899-909. 2005
- 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
- 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...
- Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Brain Res 1073:240-51. 2006
- Effects of chronic dermal exposure to nonlethal doses of methyl parathion on brain regional acetylcholinesterase and muscarinic cholinergic receptors in female rats
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...
- 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 ..
- Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic administration
Preclinical Pharmacology Section, Behavioral Neuroscience Branch, NIDA, NIH, IRP, Department of Health and Human Services, Baltimore, MD, USA
Neuropsychopharmacology 28:1281-91. 2003
- Molecular mechanisms involved in the asymmetric interaction between cannabinoid and opioid systems
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...
- 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...
- 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...
- Binding characteristics of [3H]ucb 30889 to levetiracetam binding sites in rat brain
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...
- Carvedilol blockade of rat myocardial alpha1-adrenoceptors
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...
- Antiparkinson concentrations of pramipexole and PHNO occupy dopamine D2(high) and D3(high) receptors
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...
- 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...
- Low concentrations of neuroactive steroids alter kinetics of [3H]ifenprodil binding to the NMDA receptor in rat frontal cortex
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...
- Differences in interactions with the dopamine transporter as revealed by diminishment of Na(+) gradient and membrane potential: dopamine versus other substrates
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...
- 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
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...
- [3H]linopirdine binding to rat brain membranes is not relevant for M-channel interaction
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...
- Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors
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...
- Use of [3H]fluorowillardiine to study properties of AMPA receptor allosteric modulators
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...
- Quantitative autoradiographic analysis of the new radioligand [(3)H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a]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...
- Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist
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...
- 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...
- 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...
- 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...
- Increased phencyclidine-induced hyperactivity following cortical cholinergic denervation
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...
- 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...
- Antidepressant drug induced alterations in binding to central dopamine transporter sites in the Wistar Kyoto rat strain
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
- Methylmercury elicits rapid inhibition of cell proliferation in the developing brain and decreases cell cycle regulator, cyclin E
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...
- Regional localization and developmental profile of acetylcholinesterase-evoked increases in [(3)H]-5-fluororwillardiine binding to AMPA receptors in rat brain
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...
- 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...
- Characterization of cannabinoid-binding sites in zebrafish brain
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...
- 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...
- Increase in A2A receptors in the nucleus accumbens after extended cocaine self-administration and its disappearance after cocaine withdrawal
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...
- 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...
- Brain alpha(2)-adrenoceptors in monoamine-depleted rats: increased receptor density, G coupling proteins, receptor turnover and receptor mRNA
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...
- Estrogenic activity of tamoxifen and raloxifene on rat brain AMPA receptors
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...
- Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models
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...