radioligand assay

Summary

Summary: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

Top Publications

  1. ncbi Structure-affinity relationship studies on arylpiperazine derivatives related to quipazine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor
    Andrea Cappelli
    Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
    Bioorg Med Chem 13:3455-60. 2005
  2. ncbi Changes of cooperativity between N-methylscopolamine and allosteric modulators alcuronium and gallamine induced by mutations of external loops of muscarinic M(3) receptors
    A Krejci
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
    Mol Pharmacol 60:761-7. 2001
  3. pmc Chronic nicotine exposure upregulates nicotinic receptors by a novel mechanism
    Yolanda F Vallejo
    Department of Neurobiology, Pharmacology, and Physiology, University of Chicago, Chicago, Illinois 60637, USA
    J Neurosci 25:5563-72. 2005
  4. ncbi Role of NAADP and cADPR in the induction and maintenance of agonist-evoked Ca2+ spiking in mouse pancreatic acinar cells
    Michiko Yamasaki
    Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, United Kingdom
    Curr Biol 15:874-8. 2005
  5. ncbi Development of spin-labeled probes for adenosine receptors
    Janez Ilas
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53113 Bonn, Germany
    J Med Chem 48:2108-14. 2005
  6. ncbi Consensus nomenclature for in vivo imaging of reversibly binding radioligands
    Robert B Innis
    National Institute of Mental Health, Molecular Imaging Branch, Bethesda, Maryland, USA
    J Cereb Blood Flow Metab 27:1533-9. 2007
  7. ncbi Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor
    Camilo Rojas
    Research and Translational Development, MGI PHARMA INC, 6611 Tributary St, Baltimore, MD 21224 6515, USA
    Anesth Analg 107:469-78. 2008
  8. pmc The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro
    E H Wong
    Institute of Pharmacology, Palo Alto, California 94303, USA
    Br J Pharmacol 114:851-9. 1995
  9. pmc Agonists and antagonists induce different palonosetron dissociation rates in 5-HT₃A and 5-HT₃AB receptors
    Sarah C R Lummis
    Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1QW, UK
    Neuropharmacology 73:241-6. 2013
  10. ncbi Mutational analysis of the alpha 1a-adrenergic receptor binding pocket of antagonists by radioligand binding assay
    Maruf Ahmed
    Pharmacy Department, University of Rajshahi, Rajshahi 6205, Bangladesh
    Biol Pharm Bull 31:598-601. 2008

Detail Information

Publications236 found, 100 shown here

  1. ncbi Structure-affinity relationship studies on arylpiperazine derivatives related to quipazine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor
    Andrea Cappelli
    Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
    Bioorg Med Chem 13:3455-60. 2005
    ....
  2. ncbi Changes of cooperativity between N-methylscopolamine and allosteric modulators alcuronium and gallamine induced by mutations of external loops of muscarinic M(3) receptors
    A Krejci
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
    Mol Pharmacol 60:761-7. 2001
    ....
  3. pmc Chronic nicotine exposure upregulates nicotinic receptors by a novel mechanism
    Yolanda F Vallejo
    Department of Neurobiology, Pharmacology, and Physiology, University of Chicago, Chicago, Illinois 60637, USA
    J Neurosci 25:5563-72. 2005
    ....
  4. ncbi Role of NAADP and cADPR in the induction and maintenance of agonist-evoked Ca2+ spiking in mouse pancreatic acinar cells
    Michiko Yamasaki
    Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, United Kingdom
    Curr Biol 15:874-8. 2005
    ....
  5. ncbi Development of spin-labeled probes for adenosine receptors
    Janez Ilas
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53113 Bonn, Germany
    J Med Chem 48:2108-14. 2005
    ..The novel spin-labeled A(1)-selective or A(1)/A(2B)-nonselective adenosine receptor antagonists may become useful probes for biophysicochemical investigations of adenosine receptors in their membrane environment...
  6. ncbi Consensus nomenclature for in vivo imaging of reversibly binding radioligands
    Robert B Innis
    National Institute of Mental Health, Molecular Imaging Branch, Bethesda, Maryland, USA
    J Cereb Blood Flow Metab 27:1533-9. 2007
    ..An international group of experts in pharmacokinetic modeling recommends a consensus nomenclature to describe in vivo molecular imaging of reversibly binding radioligands...
  7. ncbi Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor
    Camilo Rojas
    Research and Translational Development, MGI PHARMA INC, 6611 Tributary St, Baltimore, MD 21224 6515, USA
    Anesth Analg 107:469-78. 2008
    ..However, these attributes alone are not sufficient to explain the results with palonosetron. We sought to elucidate additional differences among 5-HT(3)-RAs that could help explain the observations in the clinic...
  8. pmc The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro
    E H Wong
    Institute of Pharmacology, Palo Alto, California 94303, USA
    Br J Pharmacol 114:851-9. 1995
    ..7 In conclusion, the functional, binding and distribution studies undertaken with the radiolabelled and non-radiolabelled RS 25259-197 (S,S enantiomer) established the profile of a highly potent and selective5-HT3 receptor antagonist...
  9. pmc Agonists and antagonists induce different palonosetron dissociation rates in 5-HT₃A and 5-HT₃AB receptors
    Sarah C R Lummis
    Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1QW, UK
    Neuropharmacology 73:241-6. 2013
    ....
  10. ncbi Mutational analysis of the alpha 1a-adrenergic receptor binding pocket of antagonists by radioligand binding assay
    Maruf Ahmed
    Pharmacy Department, University of Rajshahi, Rajshahi 6205, Bangladesh
    Biol Pharm Bull 31:598-601. 2008
    ..The results provide direct evidence that these amino acid residues are responsible for the interactions between alpha 1a-AR and radioligand [3H]prazosin as well as tamsulosin and KMD-3213...
  11. pmc Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists
    VSEVOLOD KATRITCH
    Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 53:1799-809. 2010
    ..High success rate, novelty, and diversity of the chemical scaffolds and strong ligand efficiency of the A(2A)AR antagonists identified in this study suggest practical applicability of receptor-based VLS in GPCR drug discovery...
  12. ncbi Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors: characterization by ligand binding and photoaffinity labeling
    S B Hellewell
    Unit on Receptor Biochemistry and Pharmacology, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD 20892
    Eur J Pharmacol 268:9-18. 1994
    ..These data are consistent with the notion that the 25 kDa and 21.5 kDa proteins represent sigma 1 and sigma 2 receptors, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)..
  13. ncbi PET visualization of microglia in multiple sclerosis patients using [11C]PK11195
    J C Debruyne
    Department of Neurology, Ghent University Hospital, Ghent, Belgium
    Eur J Neurol 10:257-64. 2003
    ..In conclusion, [11C]PK11195 and PET are able to demonstrate inflammatory processes with microglial involvement in MS...
  14. ncbi Allosteric interactions between the antagonist prazosin and amiloride analogs at the human alpha(1A)-adrenergic receptor
    R A Leppik
    National Institute for Medical Research, The Ridgeway, Mill Hill, London, United Kingdom
    Mol Pharmacol 57:436-45. 2000
    ....
  15. pmc Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist
    Bryan L Roth
    National Institute of Mental Health Psychoactive Drug Screening Program and Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH 44106, USA
    Proc Natl Acad Sci U S A 99:11934-9. 2002
    ..g., schizophrenia, dementia, and bipolar disorders). Additionally, these results suggest that kappa opioid receptors play a prominent role in the modulation of human perception...
  16. ncbi Transient and selective overexpression of dopamine D2 receptors in the striatum causes persistent abnormalities in prefrontal cortex functioning
    Christoph Kellendonk
    Center for Neurobiology and Behavior, College of Physicians and Surgeons, Columbia University, 1051 Riverside Drive, New York, New York 10032, USA
    Neuron 49:603-15. 2006
    ..We found that D2R overexpression in the striatum impacts dopamine levels, rates of dopamine turnover, and activation of D1 receptors in the prefrontal cortex, measures that are critical for working memory...
  17. ncbi AZD2184: a radioligand for sensitive detection of beta-amyloid deposits
    Allan E Johnson
    Disease Biology, AstraZeneca R and D, Sodertalje, Sweden
    J Neurochem 108:1177-86. 2009
    ..Taken together, the pre-clinical profile of AZD2184 in relation to the reference ligand PIB, suggests that (11)C-labeled AZD2184 is a potential radioligand for PET-visualization of beta-amyloid deposits in the living human brain...
  18. pmc The sigma1 receptor interacts with N-alkyl amines and endogenous sphingolipids
    Subramaniam Ramachandran
    Department of Pharmacology, University Wisconsin Madison, School of Medicine and Public Health, 1300 University Ave, Madison, WI 53706, USA
    Eur J Pharmacol 609:19-26. 2009
    ..The data presented here strongly supports sphingosine as an endogenous modulator of the sigma1 receptor...
  19. ncbi Generation and phenotypic analysis of sigma receptor type I (sigma 1) knockout mice
    Francina Langa
    Centro Nacional de Biotechnología CNB CSIC, Department of Molecular and Cellular Biology, Campus de Cantoblanco, 28049 Madrid, Spain
    Eur J Neurosci 18:2188-96. 2003
    ..The activity of sigma 2-receptors seems to be unaffected in sigma 1-mutant mice. These knockout mice could contribute to better understand the in vivo role of sigma-receptors...
  20. ncbi Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors
    Kevin D Burris
    Neuroscience Drug Discovery, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    J Pharmacol Exp Ther 302:381-9. 2002
    ..The receptor activity profile may underlie the unique activity of aripiprazole in animals and its antipsychotic activity in humans...
  21. ncbi A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists
    Luo Yan
    Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Kreuzbergweg 26, D 53115 Bonn, Germany
    J Med Chem 49:4384-91. 2006
    ..6 nM for the human A(2B) receptor combined with high selectivity versus the other human adenosine receptor subtypes (575-fold versus A(1), 134-fold versus A(2A), and >278-fold versus A(3))...
  22. ncbi Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones
    Anna Drabczyńska
    Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, PL 30 688 Krakow, Poland
    Eur J Med Chem 46:3590-607. 2011
    ..The new compounds, which contain a basic nitrogen atom and can therefore be protonated, may be good starting points for obtaining A(2A) antagonists with good water-solubility...
  23. ncbi 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors
    Vita Ozola
    University of Bonn, Pharmaceutical Institute Poppelsdorf, Kreuzbergweg 26, D 53115 Bonn, Germany
    Bioorg Med Chem 11:347-56. 2003
    ..Due to their high A(3) affinity, selectivity, and relatively high water-solubility, 2-phenyl-imidazo[2,1-i]purin-5-ones may become useful research tools...
  24. ncbi Synthesis and biological activity of tricyclic aryloimidazo-, pyrimido-, and diazepinopurinediones
    Anna Drabczyńska
    Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Medical College, Jagiellonian University, Medyczna 9, PL 30 688 Krakow, Poland
    Bioorg Med Chem 14:7258-81. 2006
    ..Substances with pyrimido ring displayed protective activity in ScMet or in MES and ScMet tests, showing also neurotoxicity. The pyrimidine annelated ring is beneficial for both receptor affinity and anticonvulsant activity...
  25. ncbi Different interactions between MT7 toxin and the human muscarinic M1 receptor in its free and N-methylscopolamine-occupied states
    Carole Fruchart-Gaillard
    Commissariat a l Energie Atomique, Institut de Biologie et de Tecnologies de Saclay, Service d Ingénierie Moléculaire des Protéines, Laboratoire de Toxinologie Moléculaire et Biotechnologie, Gif sur Yvette, France
    Mol Pharmacol 74:1554-63. 2008
    ..The high specificity of the MT7-M(1) receptor interaction exploits several MT7-specific residues and reveals a different mode of interaction of the toxin with the free and NMS-occupied states of the receptor...
  26. ncbi G protein-coupled receptor allosterism and complexing
    Arthur Christopoulos
    Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia
    Pharmacol Rev 54:323-74. 2002
    ..It is proposed that the study of allosteric phenomena will become of progressively greater import to the drug discovery process due to the advent of newer and more sensitive GPCR screening technologies...
  27. ncbi 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity
    Thomas Borrmann
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, D 53121 Bonn, Germany
    J Med Chem 52:3994-4006. 2009
    ..It was shown to be a useful pharmacological tool for the selective labeling of human as well as rodent A(2B) receptors (K(D) human A(2B) 0.403 nM, mouse A(2B) 0.351 nM)...
  28. ncbi Differential antagonism by conotoxin rho-TIA of contractions mediated by distinct alpha1-adrenoceptor subtypes in rat vas deferens, spleen and aorta
    Vanessa Lima
    Department of Pharmacology, Instituto de Biociencias, UNESP, Botucatu, SP 18618 000, Brazil
    Eur J Pharmacol 508:183-92. 2005
    ..It is concluded that rho-TIA will be useful for distinguishing the role of particular alpha1-adrenoceptor subtypes in native tissues...
  29. ncbi The three-finger toxin MTalpha is a selective alpha(2B)-adrenoceptor antagonist
    Katja Koivula
    Department of Biochemistry and Pharmacy, Abo Akademi University, Tykistokatu 6, FIN 20520 Turku, Finland
    Toxicon 56:440-7. 2010
    ..These findings should open up new views in terms of selective adrenoceptor drug design as well as in elucidation of alpha(2)-adrenoceptor physiology...
  30. ncbi Conformational changes that occur during M3 muscarinic acetylcholine receptor activation probed by the use of an in situ disulfide cross-linking strategy
    Stuart D C Ward
    Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Biol Chem 277:2247-57. 2002
    ..This is the first study employing an in situ disulfide cross-linking strategy to examine agonist-dependent dynamic structural changes in a G protein-coupled receptor...
  31. ncbi Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11C-PET imaging agents for beta-amyloid plaques
    Britt Marie Swahn
    Department of Medicinal Chemistry, AstraZeneca R and D Sodertalje, Sodertalje, Sweden
    Bioorg Med Chem Lett 20:1976-80. 2010
    ..It is shown that it was possible to increase the signal-to-background ratios compared to PIB 1, as demonstrated by compounds 8 and 21...
  32. ncbi Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives
    Rogier A Smits
    Leiden Amsterdam Center for Drug Research LACDR, Division of Medicinal Chemistry, Department of Pharmacochemistry, Faculty of Exact Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
    J Med Chem 49:4512-6. 2006
    ..On the basis of the derived structure-activity relationships and additional pharmacological results, a pharmacophore model was constructed, which will be the premise for the design of novel H4R ligands...
  33. pmc Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor
    Mark R Dowling
    Novartis Institutes for BioMedical Research, Wimblehurst Road, Horsham, West Sussex RH12 5AB
    Br J Pharmacol 148:927-37. 2006
    ....
  34. ncbi Characterization of AZD4694, a novel fluorinated Abeta plaque neuroimaging PET radioligand
    Anders Jureus
    Department of Neuroscience, AstraZeneca R and D Sodertalje, Sodertalje, Sweden
    J Neurochem 114:784-94. 2010
    ..v. administration. Taken together, the preclinical profile of AZD4694 suggests that fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-amyloid deposits in the living human brain...
  35. pmc Structural and functional roles of small group-conserved amino acids present on helix-H7 in the β(2)-adrenergic receptor
    Makoto Arakawa
    Department of Oral Biology, University of Manitoba, Winnipeg, MB R3E 0W4, Canada
    Biochim Biophys Acta 1808:1170-8. 2011
    ..We discuss our results in the context of van der Waals interactions of Gly315(7.42) with Trp286(6.48) and hydrogen bonding interactions of Ser319(7.46) with amino acids on H1-H2-H7 and with structural water...
  36. ncbi Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist
    Trond Ulven
    7TM Pharma A S, Fremtidsvej 3, DK 2970 Hørsholm, Denmark
    J Med Chem 48:897-900. 2005
    ..This is the first selective CRTH2 antagonist described to date, and should prove highly valuable in further elucidating the biological significance of CRTH2...
  37. pmc Longitudinal noninvasive PET-based beta cell mass estimates in a spontaneous diabetes rat model
    Fabiola Souza
    Department of Medicine, Columbia University Medical Center, New York, New York 10032, USA
    J Clin Invest 116:1506-13. 2006
    ..These studies suggest that PET-based quantitation of VMAT2 receptors provides a noninvasive measurement of BCM that could be used to study the pathogenesis of diabetes and to monitor therapeutic interventions...
  38. pmc Isolation and pharmacological characterization of AdTx1, a natural peptide displaying specific insurmountable antagonism of the alpha1A-adrenoceptor
    L Quinton
    Laboratoire des Mecanismes Reactionnels, Ecole Polytechnique, Palaiseau, France
    Br J Pharmacol 159:316-25. 2010
    ..Venoms are a rich source of ligands for ion channels, but very little is known about their capacity to modulate G-protein coupled receptor (GPCR) activity. We developed a strategy to identify novel toxins targeting GPCRs...
  39. ncbi Changes in conformation and subcellular distribution of alpha4beta2 nicotinic acetylcholine receptors revealed by chronic nicotine treatment and expression of subunit chimeras
    Patricia C Harkness
    Department of Pharmacology, University College London, London, WC1E 6BT, United Kingdom
    J Neurosci 22:10172-81. 2002
    ..The finding that subunit conformation can be influenced by coassembled subunit partners is in agreement with models of receptor assembly which propose that subunit folding continues after initial subunit-subunit interactions...
  40. ncbi Kinetic and thermodynamic assessment of binding of serotonin transporter inhibitors
    Renee S Martin
    Departments of Biochemical Pharmacology, Roche Pharmaceuticals, Palo Alto CA 94304, USA
    J Pharmacol Exp Ther 327:991-1000. 2008
    ..The fluvoxamine-type binding mode is fueled by energy released upon burying hydrophobic ligand moieties into a binding pocket that is flexible enough to suffer minimal loss in entropy from conformational constraint...
  41. ncbi Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists
    Soo Kyung Kim
    Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases NIDDK, National Institutes of Health NIH, Bethesda, Maryland 20892, USA
    J Med Chem 46:4847-59. 2003
    ..We identified new neoceptor (T88D)-neoligand pairs that were consistent with the model...
  42. ncbi Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties
    Andrea Cappelli
    Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
    J Med Chem 48:3564-75. 2005
    ....
  43. ncbi Tumor necrosis factor alpha enhances nicotinic receptor up-regulation via a p38MAPK-dependent pathway
    Lorise C Gahring
    Salt Lake City Veterans Affairs Geriatrics Research, Education, Clinical Center, Salt Lake City, Utah 84148, USA
    J Biol Chem 283:693-9. 2008
    ..This finding extends the possibilities for nAChR-inflammatory interactions in normal physiological processes and offers novel insights into endogenous mechanisms that can modify up-regulation...
  44. ncbi Allosteric uncoupling and up-regulation of benzodiazepine and GABA recognition sites following chronic diazepam treatment of HEK 293 cells stably transfected with alpha1beta2gamma2S subunits of GABA (A) receptors
    Danka Pericić
    Division of Molecular Medicine, Ruder Boskovic Institute, Laboratory for Molecular Neuropharmacology, P O Box 180, 10002 Zagreb, Croatia
    Naunyn Schmiedebergs Arch Pharmacol 375:177-87. 2007
    ..A comparable increase of [(3)H]muscimol binding sites expressed on the surface of intact HEK 293 cells suggests that internalisation of surface receptors presumably can not explain the uncoupling...
  45. ncbi Determination of folate vitamers in human serum by stable-isotope-dilution tandem mass spectrometry and comparison with radioassay and microbiologic assay
    Christine M Pfeiffer
    National Center for Environmental Health, Centers for Disease Control and Prevention, Atlanta, GA 30341, USA
    Clin Chem 50:423-32. 2004
    ....
  46. pmc Two binding sites for [3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation
    David R Owen
    Department of Experimental Medicine and Toxicology, Imperial College London, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 30:1608-18. 2010
    ..The functional significance of differences in binding characteristics warrants further investigation...
  47. ncbi Functional calcitonin gene-related peptide receptors are formed by the asymmetric assembly of a calcitonin receptor-like receptor homo-oligomer and a monomer of receptor activity-modifying protein-1
    Madeleine Heroux
    Department of Biochemistry and Groupe de Recherche Universitaire sur le Médicament, Universite de Montreal, Montreal, Quebec H3C 3J7, Canada
    J Biol Chem 282:31610-20. 2007
    ....
  48. ncbi Correlation between sigma2 receptor protein expression and histopathologic grade in human bladder cancer
    Nicola Antonio Colabufo
    Dipartimento Farmaco Chimico, Facolta di Farmacia, Universita degli Studi di Bari, Via Orabona 4, 70125 Bari, Italy
    Cancer Lett 237:83-8. 2006
    ..Moreover, these receptors were undetected in a low-grade squamous cell carcinoma and in a very rare form of anaplastic, large cells plasmacytoid cancer...
  49. ncbi Ligand-dependent differences in the internalization of endothelin A and endothelin B receptor heterodimers
    Bernd Gregan
    Institut fur Pharmakologie, Charite Universitatsmedizin Berlin, Campus Benjamin Franklin, Thielallee 67 73, 14195 Berlin, Germany
    J Biol Chem 279:27679-87. 2004
    ..Heterodimer dissociation along the endocytic pathway only occurs upon ET(B)-selective stimulation...
  50. ncbi [(11)C]PIB-amyloid binding and levels of Abeta40 and Abeta42 in postmortem brain tissue from Alzheimer patients
    Marie M Svedberg
    Uppsala University, Department of Biochemistry and Organic Chemistry, Sweden
    Neurochem Int 54:347-57. 2009
    ..Moreover, it is suggested that some of the [(11)C]PIB binding and insoluble Abeta seen in control subjects may be amyloid in the blood vessels...
  51. pmc The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors
    Jillian G Baker
    Institute of Cell Signalling, C Floor Medical School, Queen s Medical Centre, University of Nottingham, Nottingham, UK
    Br J Pharmacol 160:1048-61. 2010
    ..This study examined the affinity and intrinsic efficacy of 31 beta-adrenoceptor agonists at the three human beta-adrenoceptors to determine whether the current agonists are subtype selective because of affinity or intrinsic efficacy...
  52. 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...
  53. pmc Differential in vivo potencies of naltrexone and 6beta-naltrexol in the monkey
    M C Holden Ko
    Department of Pharmacology, University of Michigan, Ann Arbor, 48109 0632, USA
    J Pharmacol Exp Ther 316:772-9. 2006
    ....
  54. ncbi Sigma-2 receptors are specifically localized to lipid rafts in rat liver membranes
    Daniel Gebreselassie
    Unit on Receptor Biochemistry and Pharmacology, Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg 8, Rm B1 23 8 Center DR MSC 0815 Bethesda, MD 20892, USA
    Eur J Pharmacol 493:19-28. 2004
    ..Thus, sigma-2 receptors are resident in membrane lipid rafts, whereas sigma-1 receptors appear in both raft and non-raft membrane domains. Lipid rafts may play an important role in the mechanism of sigma-2 receptor-induced apoptosis...
  55. ncbi Adenine sulfate improves cardiac function and the cardiac cholinergic system after myocardial infarction in rats
    Lei Sun
    Department of Pharmacology, School of Life Science and Technology, Xi an Jiaotong University, Xi an, China
    J Pharmacol Sci 115:205-13. 2011
    ..Changes in cardiac vagal distribution density and M(2)-receptor expression raise the possibility that improvement of the cardiac cholinergic system is involved in adenine sulfate-induced cardioprotective effects...
  56. ncbi alpha-Conotoxin GI benzoylphenylalanine derivatives. (1)H-NMR structures and photoaffinity labeling of the Torpedo californica nicotinic acetylcholine receptor
    Igor E Kasheverov
    Shemyakin Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia
    FEBS J 273:1373-88. 2006
    ....
  57. ncbi Influence of 5,10-methylenetetrahydrofolate reductase polymorphism on whole-blood folate concentrations measured by LC-MS/MS, microbiologic assay, and bio-rad radioassay
    Zia Fazili
    Division of Laboratory Sciences, National Center for Environmental Health, Centers for Disease Control and Prevention, 4770 Buford Highway NE, Atlanta, GA 30345, USA
    Clin Chem 54:197-201. 2008
    ....
  58. ncbi The loop C region of the murine 5-HT3A receptor contributes to the differential actions of 5-hydroxytryptamine and m-chlorophenylbiguanide
    Asha Suryanarayanan
    Department of Chemistry and Biochemistry, The University of Alaska, Fairbanks, Alaska 99775, USA
    Biochemistry 44:9140-9. 2005
    ..Residues F226 and Y234 are important for both 5-HT and mCPBG interactions. Mutations at F226, I228, and Y234 also altered the relative efficacies of agonists, suggesting a role in the gating mechanism...
  59. ncbi International Workshop on Lessons From Animal Models for Human Type 1 Diabetes: identification of insulin but not glutamic acid decarboxylase or IA-2 as specific autoantigens of humoral autoimmunity in nonobese diabetic mice
    E Bonifacio
    Department of Medicine, Isituto Scientifico San Raffaele, Milan, Italy
    Diabetes 50:2451-8. 2001
    ..In sum, this workshop demonstrated that IAA measured by sensitive RBA are a marker of autoimmunity in NOD mice and draw into question the true nature of GADA and IA-2A in this animal model...
  60. pmc Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands
    Jillian G Baker
    Institute of Cell Signalling, School of Biomedical Sciences, Medical School, University of Nottingham, Queen s Medical Centre, Nottingham, UK
    Br J Pharmacol 159:772-86. 2010
    ..This study evaluated how the physicochemical nature of the linker and the fluorophore affected the pharmacological properties of fluorescent agonists and antagonists...
  61. ncbi Interaction of alpha-conotoxin ImII and its analogs with nicotinic receptors and acetylcholine-binding proteins: additional binding sites on Torpedo receptor
    Igor E Kasheverov
    Shemyakin Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia
    J Neurochem 111:934-44. 2009
    ....
  62. pmc Effect of the statin atorvastatin on intracellular signalling by the prostacyclin receptor in vitro and in vivo
    Sarah J O'Meara
    Department of Biochemistry, Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Belfield, Dublin 4, Ireland
    Br J Pharmacol 143:292-302. 2004
    ....
  63. pmc G-protein-coupled receptors: past, present and future
    Stephen J Hill
    Institute of Cell Signalling, University of Nottingham, Medical School, Queen s Medical Centre, Nottingham NG7 2UH
    Br J Pharmacol 147:S27-37. 2006
    ..This review provides a brief historical overview of the properties and signalling characteristics of this important family of receptors...
  64. ncbi On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2
    Jesper Mosolff Mathiesen
    7TM Pharma A S, Fremtidsvej 3, 2970 Hørsholm, Denmark
    Mol Pharmacol 69:1441-53. 2006
    ..A mechanistic understanding of insurmountability of CRTH2 antagonists could be fundamental for development of this novel class of anti-inflammatory drugs...
  65. ncbi Investigation of a functional requirement for isoprenylation by the human prostacyclin receptor
    Sinead M Miggin
    Department of Biochemistry, Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Ireland
    Eur J Biochem 269:1714-25. 2002
    ....
  66. ncbi A mechanism for rapacuronium-induced bronchospasm: M2 muscarinic receptor antagonism
    Edmund Jooste
    Department of Anesthesiology, College of Physicians and Surgeons, Columbia University, 630 West 168th Street, P and S Box 46, New York, New York 10032, USA
    Anesthesiology 98:906-11. 2003
    ..g., intubation) can result in the massive release of acetylcholine to act on unopposed M3 muscarinic receptors in airway smooth muscle, thereby facilitating bronchoconstriction...
  67. ncbi Rapacuronium augments acetylcholine-induced bronchoconstriction via positive allosteric interactions at the M3 muscarinic receptor
    Edmund H Jooste
    Department of Anesthesiology, College of Physicians and Surgeons, Columbia University, 630 West 168th Street, New York, NY 10032, USA
    Anesthesiology 103:1195-203. 2005
    ..Despite its withdrawal from clinical use, it is imperative that the mechanism by which bronchospasm occurred is understood so that new muscle relaxants introduced to clinical practice do not share these same detrimental airway effects...
  68. ncbi Synthesis and in vivo evaluation of a new PET radioligand for studying sigma-2 receptors
    Michael Kassiou
    Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Rd, Camperdown, NSW 2050, Australia
    Bioorg Med Chem 13:3623-6. 2005
    ..The evaluation of this radioligand in vivo in the mouse clearly indicates that it does not possess the required properties for studying sigma-2 receptors in the brain using PET...
  69. ncbi Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors
    Guo Min Zhao
    Department of Pharmacology, Weill Medical College of Cornell University, 1300 York Ave, New York, NY 10021, USA
    J Pharmacol Exp Ther 307:947-54. 2003
    ..The very high affinity and selectivity of [3H][Dmt1]DALDA for the mu receptor, together with its very low nonspecific binding (10-15%) and metabolic stability, make [3H][Dmt1]DALDA an ideal radioligand for labeling mu receptors...
  70. ncbi Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity
    S Lazareno
    MRC Technology, Mill Hill, London NW7 1AD, United Kingdom
    Mol Pharmacol 65:257-66. 2004
    ....
  71. 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
    ....
  72. ncbi Differences in the allosteric modulation by phenytoin of the binding properties of the sigma1 ligands [3H](+)-pentazocine and [3H]NE-100
    Enrique J Cobos
    Department of Pharmacology and Institute of Neuroscience, School of Medicine, University of Granada, 18012 Granada, Spain
    Synapse 59:152-61. 2006
    ..These results add evidence in favor of the use of phenytoin in vitro to distinguish between agonists and antagonists of sigma1 receptors...
  73. pmc Determination of cellular nicotinic acid-adenine dinucleotide phosphate (NAADP) levels
    Dev Churamani
    Department of Physiology, University College London, The Old Squash Courts, London WC1E 6BT, UK
    Biochem J 380:449-54. 2004
    ..Our improved method for the quantification of NAADP should prove useful in the further assessment of its signalling role within cells...
  74. ncbi Orally active benzoxazole derivative as 5-HT3 receptor partial agonist for treatment of diarrhea-predominant irritable bowel syndrome
    Satoshi Yoshida
    Pharmaceutical Research Department, Meiji Seika Kaisha, Ltd, 760 Morooka cho, Kohoku Ku, Yokohama 222 8567, Japan
    J Med Chem 48:7075-9. 2005
    ..Our results indicate that 5-HT(3) receptor partial agonists might be superior as therapeutic agents to the drugs currently used for IBS treatment...
  75. ncbi Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist
    Christopher J Langmead
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, Third Ave, Harlow, Essex, CM19 5AW, UK
    Mol Pharmacol 69:236-46. 2006
    ..These data provide the first direct evidence that AC-42 is an allosteric agonist that activates M(1) receptors in the absence of the orthosteric agonist...
  76. ncbi NAADP: a new second messenger for glucose-induced Ca2+ responses in clonal pancreatic beta cells
    Roser Masgrau
    Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, United Kingdom
    Curr Biol 13:247-51. 2003
    ....
  77. pmc Activity of opioid ligands in cells expressing cloned mu opioid receptors
    Parham Gharagozlou
    Department of Pharmacology, Molecular Research Institute, Mountain View, CA 94043, USA
    BMC Pharmacol 3:1. 2003
    ..Efficacies and potencies of these ligands were determined relative to the endogenous ligand beta-endorphin and the common mu agonist, morphine...
  78. ncbi Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2
    Aaron N Hata
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232 2372, USA
    Mol Pharmacol 67:640-7. 2005
    ..Together, these results reveal structural features of arylacetic acid NSAIDs that may be exploited for the development of selective CRTH2 ligands...
  79. ncbi Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells
    Enrique J Cobos
    Department of Pharmacology and Institute of Neuroscience, Faculty of Medicine, University of Granada, Granada, Spain
    J Neurochem 102:812-25. 2007
    ..These results suggest that HP may irreversibly inactivate sigma(1) receptors in guinea pig and human cells, probably after metabolism to reduced HP...
  80. ncbi Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human beta1-adrenoceptor
    Jillian G Baker
    Institute of Cell Signaling, Queen s Medical Centre, Nottingham, NG7 2UH, UK
    Mol Pharmacol 74:1246-60. 2008
    ..Modeling studies provide a basis for these overlapping sites with either the tert-butylamino group or the hydroxyethyloxy and imidazolone portions of CGP 12177 capable of forming polar interactions with Asp138 and Asn363...
  81. ncbi Discovery of an ectopic activation site on the M(1) muscarinic receptor
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, San Diego, California 92121, USA
    Mol Pharmacol 61:1297-302. 2002
    ....
  82. ncbi New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells
    Richard J Middleton
    School of Pharmacy, Centre for Biomolecular Sciences, and School of Chemistry, University of Nottingham, University Park, Nottingham, United Kingdom
    J Med Chem 50:782-93. 2007
    ....
  83. pmc The effects of the statins lovastatin and cerivastatin on signalling by the prostanoid IP-receptor
    O A Lawler
    Department of Biochemistry, Conway Institute of Biomolecular and Biomedical Research, Merville House, University College Dublin, Belfield, Dublin 4, Ireland
    Br J Pharmacol 132:1639-49. 2001
    ....
  84. ncbi Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD)
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 45:4344-9. 2002
    ..The incorporation of isomeric dialkylazetidines into other biologically active molecules may be a useful strategy to model the active conformations of dialkylamines and dialkylamides...
  85. pmc Identification of specific calcitonin-like receptor residues important for calcitonin gene-related peptide high affinity binding
    Sugato Banerjee
    Department of Pharmacology, Physiology and Therapeutics, School of Medicine and Health Sciences, University of North Dakota, Grand Forks, ND 58202 9037, USA
    BMC Pharmacol 6:9. 2006
    ..Therefore, we hypothesize that hydrophobic amino acids within the previously characterized 18 amino acid CLR N-terminus domain are important binding contacts for the C-terminal phenylalaninamide of CGRP...
  86. pmc Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor
    Anikó Göblyös
    Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, Leiden University, P O Box 9502, 2300 RA, Leiden, The Netherlands
    J Med Chem 49:3354-61. 2006
    ..Thus, we have prepared allosteric enhancers of the human A3AR that have an improved allosteric effect in comparison to the inhibition of equilibrium binding at the orthosteric site...
  87. ncbi Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary
    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, USA
    J Med Chem 45:4471-84. 2002
    ..Thus, A(3)AR activation appeared to require flexibility at the 5'- and 3'-positions, which was diminished in (N)-methanocarba, spiro, and epoxide analogues, and was characteristic of ribose interactions at TM6 and TM7...
  88. ncbi Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation
    Sinead M Miggin
    Department of Biochemistry, Conway Institute of Biomolecular and Biomedical Research, Merville House, University College Dublin, Belfield, Dublin 4, Ireland
    J Biol Chem 278:6947-58. 2003
    ....
  89. ncbi Synthesis and evaluation of radiolabeled antagonists for imaging of beta-adrenoceptors in the brain with PET
    Petra Doze
    PET Center, Groningen University Hospital, P O Box 30 001, 9700 RB Groningen, The Netherlands
    Neurochem Int 40:145-55. 2002
    ..Apparently, the criteria of a high affinity and a moderately high lipophilicity were insufficient to predict the suitability of beta-adrenergic antagonists for visualization of beta-adrenoceptors in the central nervous system...
  90. ncbi Dopamine D2 receptor-deficient mice exhibit decreased dopamine transporter function but no changes in dopamine release in dorsal striatum
    S D Dickinson
    Department of Pharmacology, University of Colorado Health Sciences Center, Denver 80262, USA
    J Neurochem 72:148-56. 1999
    ..These results further strengthen the idea that the D2 DA receptor subtype modulates activity of the striatal DAT...
  91. ncbi Binding properties of the novel, non-peptide CGRP receptor antagonist radioligand, [(3)H]BIBN4096BS
    Marcus Schindler
    Department of Cardiovascular Research I, Boehringer Ingelheim Pharma KG, Birkendorfer Strasse 65, 88397 Biberach, Germany
    Eur J Pharmacol 442:187-93. 2002
    ..099 nM. These data, using [(3)H]BIBN4096BS, confirm the high affinity of this novel antagonist for the primate CGRP receptor and demonstrate furthermore that this radioligand is a useful tool to study CGRP receptor pharmacology...
  92. ncbi Evidence for a tandem two-site model of ligand binding to muscarinic acetylcholine receptors
    J Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, 14220 Prague, Czech Republic and the University of Minnesota Medical School, Minneapolis, Minnesota 55455, USA
    J Biol Chem 275:18836-44. 2000
    ..The peripheral subsite of M(1) receptors may include Asp-99. Experimental data on [(3)H]NMS and [(3)H]QNB association and dissociation perfectly agree with the predictions of the tandem two-site model...
  93. ncbi Characterization of haloperidol and trifluperidol as subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonists using [3H]TCP and [3H]ifenprodil binding in rat brain membranes
    L L Coughenour
    Department of Neurological and Neurodegenerative Disease, Parke Davis Pharmaceutical Research, Ann Arbor, Michigan 48105, USA
    J Pharmacol Exp Ther 280:584-92. 1997
    ....
  94. ncbi 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors
    R A Glennon
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia 23298, USA
    J Med Chem 43:1011-8. 2000
    ..e., 10: K(i) = 20 nM) but lacks agonist character. 2-Substituted tryptamines, then, might allow entry to a novel class of 5-HT(6) agonists and antagonists...
  95. ncbi Subtype selectivity of the positive allosteric action of alcuronium at cloned M1-M5 muscarinic acetylcholine receptors
    J Jakubik
    Institute of Physiology, Academy of Sciences of the Czech Republic, Prague
    J Pharmacol Exp Ther 274:1077-83. 1995
    ....
  96. ncbi Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter
    Jianjing Cao
    Medicinal Chemistry and Psychobiology Sections, Intramural Research Program, National Institute on Drug Abuse, 5500 Nathan Shock Drive, Baltimore, Maryland 21224, USA
    J Med Chem 47:6128-36. 2004
    ....
  97. ncbi Fluorinated diaryl sulfides as serotonin transporter ligands: synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents
    Yiyun Huang
    Department of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, New York, New York 10032, USA
    J Med Chem 48:2559-70. 2005
    ..Among these four ligands, three appear to be promising radioligands suitable for the labeling of SERT in vivo, with 18a providing a higher specific binding in vivo than 16 or 18b...
  98. ncbi Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells
    Shanti Kalipatnapu
    Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500007, India
    Biosci Rep 24:101-15. 2004
    ....
  99. ncbi Synthesis and receptor binding of new thieno[2,3-d]-pyrimidines as selective ligands of 5-HT(3) receptors
    Maria N Modica
    Dipartimento di Scienze Farmaceutiche, Universita di Catania, Catania, Italy
    Arch Pharm (Weinheim) 341:333-43. 2008
    ..Its binding interactions with 5-HT(3A )receptors were analysed by using receptor modelling and comparative docking...
  100. ncbi Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization
    Morley D Hollenberg
    Department of Pharmacology and Therapeutics, University of Calgary Faculty of Medicine, 3330 Hospital Drive NW, Calgary, AB T2N4N1, Canada
    J Pharmacol Exp Ther 326:453-62. 2008
    ..We conclude that ornithine-derivatized 2fLI peptides are conveniently synthesized PAR2 probes that will be of value for future studies of receptor binding and visualization...
  101. ncbi Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles
    Karin Schlotter
    Department of Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstrasse 19, D 91052 Erlangen, Germany
    J Med Chem 48:3696-9. 2005
    ..50 nM) and dopamine D3 receptor binding (1b, 0.64 nM) and selective D4 agonist properties of the ruthenocene 1c may be a starting point for highly beneficial central nervous system active drugs...

Research Grants65

  1. Neuroactive Steroid GABAA Receptor Positive Modulators for Fragile X Syndrome
    Albert J Robichaud; Fiscal Year: 2013
    ..Compound screening will include, a radioligand assay to confirm target engagement, electrophysiology studies of synaptic and extra-synaptic GABAA receptor ..
  2. STRUCTURAL BASIS FOR DIFFERENCES BETWEEN ELH AND ECG
    GEORGE BOUSFIELD; Fiscal Year: 1999
    ..The activities of these hybrids will be tested in a rat testis LH radioligand assay, rat testis Leydig cell steroidogenesis assay in vitro and in an in vivo eCG bioassay...
  3. NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTION
    Frank Carroll; Fiscal Year: 2008
    ..abstract_text> ..
  4. COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTION
    Frank Carroll; Fiscal Year: 2007
    ..abstract_text> ..
  5. Design and Development of Pharmacotherapies for Treating Stimulant Abuse
    Frank Ivy Carroll; Fiscal Year: 2010
    ..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
  6. NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCE
    Frank Carroll; Fiscal Year: 2001
    ..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
  7. Fetal & Adolescent Nicotine Effects on CNS 5HT Systems
    Theodore Slotkin; Fiscal Year: 2003
    ..abstract_text> ..
  8. MECHANISMS OF CHLORPYRIFOS DEVELOPMENTAL NEUROTOXICITY
    Theodore Slotkin; Fiscal Year: 2004
    ..Molecular mechanisms of developmental neurotoxicity can be determined and linked to eventual alterations in behavioral performance. ..
  9. DRUGS AND DEVELOPMENT OF THE ADRENERGIC NERVOUS SYSTEM
    Theodore Slotkin; Fiscal Year: 2003
    ....
  10. SYNTHETIC SUBSTANCES CONTROLLING REPRODUCTION
    Jean Rivier; Fiscal Year: 2005
    ..Such molecules are not presently available to academic researchers. As in the past twenty years, collaborations with academic colleagues will be initiated, to maximize the impact of this research. ..
  11. AMINOBENZOMORPHAN: POTENTIAL COCAINE ABUSE MEDICATIONS
    Mark Wentland; Fiscal Year: 2009
    ..Radioligand binding, [35S]GTPvS, and mouse antinociceptive assays will be used to characterize new targets pharmacologically. ..
  12. Somatostatin Receptor-Selective Agonists and Antagonists
    Jean Rivier; Fiscal Year: 2006
    ..abstract_text> ..
  13. 2,5 CYCLOHEXADIENONES IN NATURAL PRODUCTS SYNTHESIS
    Mark Wentland; Fiscal Year: 2001
    ....
  14. A3 Adenosine Receptors Cardioprotective Mechanisms
    John Auchampach; Fiscal Year: 2007
    ..The results of theses studies should also provide new insights into the therapeutic utility of targeting A3ARs in patients with ischemic heart disease. ..
  15. DESIGN OF INHIBITORS OF EPINEPHRINE BIOSYNTHESIS
    GARY GRUNEWALD; Fiscal Year: 2005
    ..These inhibitors will be the first pharmacological tools available to help determine the function(s) of Epi in the CNS. This project is ripe and ready to burst forth with important new results. ..
  16. Small Animal PET (microPET)
    JOGESH MUKHERJEE; Fiscal Year: 2007
    ..abstract_text> ..
  17. SPECIFIC PROBES FOR THE ER HORMONE BINDING DOMAIN
    Robert Hanson; Fiscal Year: 2002
    ..The conclusions will aid in the design of better second generation ligands and the development of a better hypothesis for the interactions of the hormone-receptor-effector complex. ..
  18. Radiotracer R and D in Nuclear Medicine and Neuroscience
    Yu Shin Ding; Fiscal Year: 2006
    ..abstract_text> ..
  19. STEREOCHEMICAL ASPECTS OF HALLUCINOGENESIS
    David Nichols; Fiscal Year: 2007
    ..These studies may lead to a rat model of schizophrenia that could be very useful in developing and understanding new types of antipsychotic agents. ..
  20. Evaluation of Vitamin D Requirements During Pregnancy
    Bruce Hollis; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  21. New PET radioligand for the serotonin transporter
    Yiyun Huang; Fiscal Year: 2007
    ..Introduction of [18F]AFM would constitute the first PET tracer for the SERT that can be prepared in a central facility and distributed to various sites for clinical imaging purposes. ..
  22. Hybrid Drugs: Novel Pharmacotherapy for ADHD
    FRANK TARAZI; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  23. The Neuroanatomy of Antipsychotic Drug Action
    WILLIAM FRANKLE; Fiscal Year: 2008
    ..abstract_text> ..
  24. Development of PET radioligands for cerebral cannabinoid receptor (CB1)
    ANDREW HORTI; Fiscal Year: 2008
    ....
  25. HISTAMINERGIC MECHANISMS OF ANTINOCICEPTION
    LINDSAY HOUGH; Fiscal Year: 2009
    ..abstract_text> ..
  26. The Effects of Cannabis Use/Abuse on In Vivo Dopamine Function
    WILLIAM FRANKLE; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  27. Role of the Amygdala in Opioid Self-administration in Rats with Chronic Pain.
    Thomas Martin; Fiscal Year: 2009
    ....
  28. STEREOCHEMICAL ASPECTS OF HALLUCINOGENESIS
    David Nichols; Fiscal Year: 2008
    ..abstract_text> ..
  29. PHARMACOKINETICS AND FETAL EXPOSURE TO NARCOTICS
    Hazel Szeto; Fiscal Year: 2002
    ..The proposed studies will provide new information on the functional roles of opiate receptor subtypes in the fetus, and should be helpful in the design of better analgesics for perinatal use. ..
  30. Evaluation in Primates of Cocaine Esterase for the Treatment of Cocaine Toxicity
    Mei Chuan Ko; Fiscal Year: 2010
    ..Dose-response functions for each enzyme will be obtained repeatedly and blood samples analyzed for titer development so that tolerance to the effects of CocE can be monitored. ..
  31. Establishing the Vitamin D Requirements During Lactation
    Bruce W Hollis; Fiscal Year: 2010
    ..The findings of this study will generate important new information for health care professionals and policy makers with regard to vitamin D requirements and the potential benefit to both mother and infant. ..
  32. EICOSANOIDS AND PULMONARY VASCULAR TONE
    SANDRA PFISTER; Fiscal Year: 2002
    ....
  33. Mitoprotective and antioxidant peptides for DM treatment
    Hazel Szeto; Fiscal Year: 2006
    ..abstract_text> ..
  34. Discovery of Novel Pharmacotherapies: Cocaine Dependence
    PETER MELTZER; Fiscal Year: 2008
    ..vi) analogues of pyrovalerone. ..
  35. 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. ..
  36. Selective Prenatal Dopamine Damage in Non Human Primates
    John Elsworth; Fiscal Year: 2003
    ..Thus, the proposed work may lead ultimately to an animal model for one or more pediatric brain disorders. ..
  37. New PET Radiotracers-Monoamine Transporters
    Michael Kilbourn; Fiscal Year: 2003
    ....
  38. 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. ..
  39. DEVELOPMENT OF POTENTIALLY SELECTIVE DOPAMINE AGONISTS
    David E Nichols; Fiscal Year: 2010
    ..Our work will generate molecular probes that should help to increase our understanding of these pathways, and may also provide new therapies for disorders such as Parkinson's disease and schizophrenia. ..
  40. 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. ..
  41. Cell-Permeable Peptides for Mitochondrial Protection
    Hazel Szeto; Fiscal Year: 2005
    ..Potential collaborators for the animal studies have already been identified. ..
  42. Treatments for Nicotine Dependence: Brain Mechanisms
    Arthur Brody; Fiscal Year: 2005
    ..abstract_text> ..
  43. Intrathecal Opioid-Induced Pruritus
    Mei Chuan Ko; Fiscal Year: 2003
    ..These studies would provide a systematic understanding of the pharmacology of intrathecal morphine-induced pruritus in primates and establish the basis for identifying potential therapeutically effective antipruritics. ..
  44. NON-OPIOID ANALGESICS DERIVED FROM IMPROGAN
    LINDSAY HOUGH; Fiscal Year: 2006
    ..These experiments will help to discover the mechanism of action of this novel class of agents, and lead to the development of new pharmacotherapies for pain. ..
  45. Cell Growth Inhibiton and Estrogen Action
    Barry Markaverich; Fiscal Year: 2004
    ..The proposed studies should precisely define specific effects of MeHPLA and bioflavonoids on chromatin structure and function, growth related gene transcription and cellular proliferation in normal and malignant cells. ..
  46. Protein Kinase in Opioid Receptor Regulation & Tolerance
    BYRON YOBURN; Fiscal Year: 2003
    ..As such, these results may provide important insights for developing strategies to treat opioid drug abuse and pain. ..
  47. NOVEL NONPEPTIDE LIGANDS FOR THE OPIOID RECEPTORS
    Subramaniam Ananthan; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  48. TREATMENT OF NEGATIVE SYMPTOMS AND COGNITIVE IMPAIRMENTS
    Daniel Javitt; Fiscal Year: 2003
    ..The study will provide new information on the efficacy of d-cycloserine and glycine for both persistent primary and secondary negative symptoms and its effect on cognitive functioning. ..
  49. Synthesis and Evaluation of Sigma-Active Cocaine Antagonists
    Rae R Matsumoto; Fiscal Year: 2010
    ..It is anticipated that the results of this project will stimulate the rational development of new a2 receptor probes and ultimately contribute to improved treatments for psychostimulant abuse. ..
  50. Brain Cannabinoid Signaling: Selectivity and Adaptation
    Laura J Sim Selley; Fiscal Year: 2010
    ..This project will determine roles of specific signaling proteins in the effects of acute and long-term CB1R activation by THC and are relevant to cannabinoid therapeutics and drug abuse. ..
  51. Methylphenidate-Ethanol Interaction in ADHD and Coabuse
    Kennerly Patrick; Fiscal Year: 2003
    ..g., dextroamphetamine vs. MPH; dI-MPH vs. d-MPH; immediate-release MPH vs. extended-release MPH; or adjustment of MPH. ..
  52. Imaging agents of norepinephrine transporters
    HANK KUNG; Fiscal Year: 2007
    ..abstract_text> ..
  53. Serotonin Modulation in Geriatric Depression
    Gwenn Smith; Fiscal Year: 2006
    ..abstract_text> ..
  54. Prion Transport Across the Blood-Brain Barrier
    William Banks; Fiscal Year: 2009
    ..To cause disease, prions must cross the blood-brain barrier to enter the brain. We will determine how prions cross the BBB. Knowing how prions enter the brain should lead to strategies on how to prevent prion diseases. ..
  55. STUDIES OF NATURAL PRODUCTS BY CHIROPTICAL METHODS
    Koji Nakanishi; Fiscal Year: 2004
    ..This will include CD studies of retinal/opsin in rhodopsin and retinal/bacterioopsin in bacteriorhodopsin. Vinca alkaloid/tubulin and taxoid/tubulin complexes will be analyzed by FDCD. ..
  56. TREATMENT FOR ALCHOLISM: A PRIMATE MODEL
    KELLY COSGROVE; Fiscal Year: 2002
    ..Thus, the effects of bremazocine and naltrexone on ethanol self-administration as a function of sex will be investigated. ..
  57. Cyclotron for PET Isotope Production
    Kenneth Krohn; Fiscal Year: 2002
    ..This cyclotron will be a productive research tool at UW for at least 20 years, well beyond the lifetime of most high-end instrumentation. ..
  58. COCAINE SELF ADMINISTRATION IN DOPAMINE KNOCKOUT MICE
    SIMON CAINE; Fiscal Year: 2003
    ..abstract_text> ..
  59. SP004, a sigma-1 ligand with AchE inhibition properties
    Laurent Lecanu; Fiscal Year: 2004
    ..Our goal in this Phase I STTR application is to prove the concept that a dual activity compound, such as SP004, is efficacious in an in vivo settings simulating human neuropathology. ..
  60. Dopamine D3 Receptor Imaging Agents for PET and SPECT
    Robert Mach; Fiscal Year: 2006
    ..A secondary goal of this project is to develop an iodine-125 labeled radiotracer for in vitro binding studies of the D3 receptor. ..
  61. PET Radiotracers for Imaging Apoptosis
    Robert Mach; Fiscal Year: 2004
    ..If successful, the research described in this research proposal will provide a PET-based imaging procedure for measuring apoptosis that will be of tremendous value to the PET research community. ..
  62. Biochemical analysis of the human vs. mouse Ah receptor
    Gary Perdew; Fiscal Year: 2007
    ..Collectively, these studies will establish the level of divergence in human vs. mouse AhR function and should allow a better assessment of the significance of human exposure to TCDD. [unreadable] [unreadable] [unreadable]..
  63. Effects of intracellular angiotensin II
    Julia Cook; Fiscal Year: 2009
    ..abstract_text> ..