H Donald Burns

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development
    H D Burns
    Department of Pharmacology, Merck Research Laboratories, WP44C 2, Sumneytown Pike, West Point, PA 19438, USA
    Curr Opin Chem Biol 3:388-94. 1999
  2. ncbi request reprint Screening cascade and development of potential Positron Emission Tomography radiotracers for mGluR5: in vitro and in vivo characterization
    Shil Patel
    Imaging Research and Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA
    Mol Imaging Biol 7:314-23. 2005
  3. pmc [18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor
    H Donald Burns
    Imaging Research, Merck Research Laboratories, West Point, PA 19486, USA
    Proc Natl Acad Sci U S A 104:9800-5. 2007
  4. doi request reprint Inverse agonist histamine H3 receptor PET tracers labelled with carbon-11 or fluorine-18
    Terence G Hamill
    Merck Research Laboratories, Discovery Imaging Department, West Point, Pennsylvania 19486, USA
    Synapse 63:1122-32. 2009
  5. doi request reprint PET imaging studies in rhesus monkey with the cannabinoid-1 (CB1) receptor ligand [11C]CB-119
    Terence G Hamill
    Merck Research Laboratories, Imaging Research Department, WP44C 2, West Point, PA 19486, USA
    Mol Imaging Biol 11:246-52. 2009
  6. doi request reprint Evaluation of [¹⁸F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, PA 19486, USA
    Neuroimage 68:1-10. 2013
  7. doi request reprint Synthesis, characterization, and monkey PET studies of [¹⁸F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Synapse 65:125-35. 2011
  8. doi request reprint Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain
    Sandra Marina Sanabria-Bohórquez
    Imaging, Merck Research Laboratories, Sumneytown Pike WP44D 2, West Point, PA 19486, USA
    Eur J Nucl Med Mol Imaging 37:920-33. 2010
  9. ncbi request reprint Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers
    Terence G Hamill
    Merck Research Laboratories, Imaging Research Department, West Point, PA 19486, USA
    Synapse 56:205-16. 2005
  10. doi request reprint Synthesis, characterization, and monkey positron emission tomography (PET) studies of [18F]Y1-973, a PET tracer for the neuropeptide Y Y1 receptor
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, PA 19486, USA
    Neuroimage 54:2635-42. 2011

Detail Information

Publications25

  1. ncbi request reprint Positron emission tomography neuroreceptor imaging as a tool in drug discovery, research and development
    H D Burns
    Department of Pharmacology, Merck Research Laboratories, WP44C 2, Sumneytown Pike, West Point, PA 19438, USA
    Curr Opin Chem Biol 3:388-94. 1999
    ....
  2. ncbi request reprint Screening cascade and development of potential Positron Emission Tomography radiotracers for mGluR5: in vitro and in vivo characterization
    Shil Patel
    Imaging Research and Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA
    Mol Imaging Biol 7:314-23. 2005
    ..Use of mGluR5 receptor radiotracers to determine whether an in vitro binding assay is able to predict how good a radiotracer is likely to be in imaging receptor in the central nervous system (CNS) via positron emission tomography (PET)...
  3. pmc [18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor
    H Donald Burns
    Imaging Research, Merck Research Laboratories, West Point, PA 19486, USA
    Proc Natl Acad Sci U S A 104:9800-5. 2007
    ..In addition, it allows demonstration of target engagement and noninvasive dose-occupancy studies to aid in dose selection for clinical trials of CB1R inverse agonists...
  4. doi request reprint Inverse agonist histamine H3 receptor PET tracers labelled with carbon-11 or fluorine-18
    Terence G Hamill
    Merck Research Laboratories, Discovery Imaging Department, West Point, Pennsylvania 19486, USA
    Synapse 63:1122-32. 2009
    ..These tracers are very promising candidates as clinical PET tracers to both study the histamine H3R system and measure receptor occupancy of H3R therapeutic compounds...
  5. doi request reprint PET imaging studies in rhesus monkey with the cannabinoid-1 (CB1) receptor ligand [11C]CB-119
    Terence G Hamill
    Merck Research Laboratories, Imaging Research Department, WP44C 2, West Point, PA 19486, USA
    Mol Imaging Biol 11:246-52. 2009
    ..The in vitro and in vivo evaluation of the selective, high affinity (human CB1 IC(50) 0.49 nM) inverse agonist CB1R tracer [(11)C]CB-119, a close analog of the previously disclosed [(18)F]MK-9470, was undertaken...
  6. doi request reprint Evaluation of [¹⁸F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, PA 19486, USA
    Neuroimage 68:1-10. 2013
    ..Additionally, [(18)F]MK-0911 may be a useful tool for studying the pharmacology of ORL1 in various human populations and disease states...
  7. doi request reprint Synthesis, characterization, and monkey PET studies of [¹⁸F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Synapse 65:125-35. 2011
    ..Taken together, these results are promising for clinical PET studies with [¹⁸F]MK-1312 to determine mGluR1 occupancy of MK-5435...
  8. doi request reprint Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain
    Sandra Marina Sanabria-Bohórquez
    Imaging, Merck Research Laboratories, Sumneytown Pike WP44D 2, West Point, PA 19486, USA
    Eur J Nucl Med Mol Imaging 37:920-33. 2010
    ..Quantitative imaging of the type 1 cannabinoid receptor (CB1R) opens perspectives for many neurological and psychiatric disorders. We characterized the kinetics and reproducibility of the CB1R tracer [(18)F]MK-9470 in human brain...
  9. ncbi request reprint Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers
    Terence G Hamill
    Merck Research Laboratories, Imaging Research Department, West Point, PA 19486, USA
    Synapse 56:205-16. 2005
    ..In vivo metabolism studies showed 3b to be long-lived in rhesus plasma with only one other more polar metabolite observed...
  10. doi request reprint Synthesis, characterization, and monkey positron emission tomography (PET) studies of [18F]Y1-973, a PET tracer for the neuropeptide Y Y1 receptor
    Eric D Hostetler
    Imaging, Merck Research Laboratories, West Point, PA 19486, USA
    Neuroimage 54:2635-42. 2011
    ..18)F]Y1-973 is a suitable PET tracer for imaging NPY Y1 in rhesus monkey with potential for translation to human PET studies...
  11. ncbi request reprint Image-derived input function for [11C]flumazenil kinetic analysis in human brain
    Sandra M Sanabria-Bohórquez
    Imaging Research, Merck Research Laboratories, West Point, PA, USA
    Mol Imaging Biol 5:72-8. 2003
    ..We describe a method for analysis of [11C]flumazenil data using an input curve directly derived from the positron emission tomography (PET) images...
  12. doi request reprint The synthesis and preclinical evaluation in rhesus monkey of [¹⁸F]MK-6577 and [¹¹C]CMPyPB glycine transporter 1 positron emission tomography radiotracers
    Terence G Hamill
    Discovery Imaging, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Synapse 65:261-70. 2011
    ..Of these two tracers, [¹⁸F]MK-6577 was more extensively characterized and is a promising clinical positron emission tomography tracer for imaging GlyT1 and for measuring GlyT1 occupancy of therapeutic compounds...
  13. doi request reprint The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake
    Carol Addy
    Merck Research Laboratories, Boston, MA 02115, USA
    Cell Metab 7:68-78. 2008
    ..Mechanism-of-action studies suggest that engagement of the CB1R by taranabant leads to weight loss by reducing food intake and increasing energy expenditure and fat oxidation...
  14. ncbi request reprint A remote-controlled high pressure reactor for radiotracer synthesis with [11C]carbon monoxide
    Eric D Hostetler
    Merck Research Laboratories, PO Box 4 WP44C 2, West Point, Pennsylvania 19486, USA
    Nucl Med Biol 29:845-8. 2002
    ..For example, AMPA receptor modulator [11C]CX546 was synthesized from its respective precursors in 37% isolated yield, uncorrected from trapped [11C]CO...
  15. ncbi request reprint The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine
    Peter Lin
    Department of Medicinal Chemistry, Merck and Co Inc, PO Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 17:5191-8. 2007
    ..An in vivo rhesus macaque brain receptor occupancy PET study for compound 45b revealed an estimated Occ(90) approximately 300 ng/ml...
  16. ncbi request reprint An in vitro assay for predicting successful imaging radiotracers
    Shil Patel
    Imaging Research and Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA
    Mol Imaging Biol 5:65-71. 2003
    ..To develop an in vitro binding assay able to predict whether a radiolabel is likely to be a useful clinical tracer for positron emission tomography (PET)...
  17. ncbi request reprint A cell-based radioligand binding assay for farnesyl: protein transferase inhibitors
    Robert B Lobell
    Department of Cancer Research, West Point, PA 19486, USA
    J Biomol Screen 8:430-8. 2003
    ..Similar methods could be employed in the optimization of inhibitors for other intracellular drug targets...
  18. ncbi request reprint Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant
    Mats Bergstrom
    Uppsala Positron Emission Tomography Centre, Uppsala, Sweden
    Biol Psychiatry 55:1007-12. 2004
    ....
  19. ncbi request reprint Synthesis and characterization of a potent, selective, radiolabeled substance-P antagonist for NK1 receptor quantitation: ([18F]SPA-RQ)
    Olof Solin
    Turku PET Centre, Turku, Finland
    Mol Imaging Biol 6:373-84. 2004
    ..To develop and characterize a radiolabelled Substance-P antagonist useful for quantitation of neurokinin-1 receptors in the brain via PET imaging...
  20. ncbi request reprint Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults
    Ngozi Erondu
    Merck and Co, Inc, 126 E Lincoln Avenue, Rahway, New Jersey 07065
    Cell Metab 4:275-82. 2006
    ..These observations provide the first clinical insight into the human NPY-energy homeostatic pathway and suggest that solely targeting the NPY5R in future drug development programs is unlikely to produce therapeutic efficacy...
  21. ncbi request reprint Human biodistribution and radiation dosimetry of the tachykinin NK1 antagonist radioligand [18F]SPA-RQ: comparison of thin-slice, bisected, and 2-dimensional planar image analysis
    David R Sprague
    Molecular Imaging Branch, NIMH, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 48:100-7. 2007
    ..The aims of this study were to estimate the radiation safety profile and relative risks of [(18)F]SPA-RQ with 3 different methods of image analysis...
  22. doi request reprint In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-a partial agonist
    Koen Van Laere
    Division of Nuclear Medicine, K U Leuven, Belgium
    Biol Psychiatry 64:153-61. 2008
    ....
  23. doi request reprint Whole-body biodistribution and radiation dosimetry of the human cannabinoid type-1 receptor ligand 18F-MK-9470 in healthy subjects
    Koen Van Laere
    Division of Nuclear Medicine, University Hospital and K U Leuven, Leuven, Belgium
    J Nucl Med 49:439-45. 2008
    ..We have used whole-body PET/CT to characterize the biodistribution and dosimetry of a novel high-affinity, subtype-selective radioligand, (18)F-MK-9470, in healthy male and female subjects...
  24. ncbi request reprint Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use
    Ping Liu
    J Med Chem 50:3427-30. 2007
    ..Further optimization focused on reducing the lipophilicity and increasing the CB1R affinity. These efforts led to the identification of [18F]-16 that exhibited good brain uptake and an excellent signal-to-noise ratio in rhesus monkeys...
  25. ncbi request reprint [Re symposium: "Approaches to optimize the discovery of CNS receptor imaging probes for use in drug discovery and development"]
    Rikki N Waterhouse
    Mol Imaging Biol 5:347-9. 2003