Merck Research Laboratories

Summary

Organization: Merck Research Laboratories
Country: USA

Top Publications

  1. doi Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments
    Joseph M Metzger
    Departments of Pharmacology, Rahway, NJ 07065, USA
    Am J Physiol Endocrinol Metab 299:E816-24. 2010
  2. ncbi Assessment of female and male fertility in Sprague-Dawley rats administered vorinostat, a histone deacetylase inhibitor
    L David Wise
    Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Birth Defects Res B Dev Reprod Toxicol 83:19-26. 2008
  3. ncbi Mini review on molecular modeling of P-glycoprotein (Pgp)
    Sookhee N Ha
    Basic Chemistry, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Curr Top Med Chem 7:1525-9. 2007
  4. ncbi Application of PCR technology in vaccine product development
    Jayanthi J Wolf
    Merck Research Laboratories, Biologics Safety Assessment, Merck and Co, Inc, PO Box 4, WP45 338, West Point, PA 19486, USA
    Expert Rev Vaccines 6:547-58. 2007
  5. ncbi Highly selective cascade couplings for the syntheses of functionalized piperidinones and bispidines
    Feng Xu
    Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA
    Org Lett 9:2669-72. 2007
  6. ncbi Isolation and structure of platencin: a FabH and FabF dual inhibitor with potent broad-spectrum antibiotic activity
    Hiranthi Jayasuriya
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
    Angew Chem Int Ed Engl 46:4684-8. 2007
  7. ncbi A practical synthesis of a gamma-secretase inhibitor
    Jeremy P Scott
    Department of Process Research, Merck Sharp and Dohme Research Laboratories, Hertford Road, Hoddesdon, Hertfordshire EN11 9BU, U K
    J Org Chem 72:4149-55. 2007
  8. pmc Establishing acceptance criteria for cell-mediated-immunity assays using frozen peripheral blood mononuclear cells stored under optimal and suboptimal conditions
    Jeffrey G Smith
    Vaccine and Biologics Research, Merck Research Laboratories, WP26B 1144, Merck and Co, Inc, 770 Sumneytown Pike, West Point, PA 19486, USA
    Clin Vaccine Immunol 14:527-37. 2007
  9. ncbi One-step synthesis of alpha-chloro acetophenones from acid chlorides and aryl precursors
    Jonathan Rosen
    Merck and Company, Inc, Department of Process Research, P O Box 2000, Rahway, New Jersey 07065, USA
    Org Lett 9:667-9. 2007
  10. ncbi A generally applicable method for assessing the electrophilicity and reactivity of diverse nitrile-containing compounds
    Renata M Oballa
    Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Highway, Kirkland, Que, Canada H9H 3L1
    Bioorg Med Chem Lett 17:998-1002. 2007

Research Grants

  1. Keystone Symposium: Eicosanoid Lipid Mediators
    Jilly Evans; Fiscal Year: 2003
  2. The Molecular and Integrative Basis for Toxic Responses
    Roger Ulrich; Fiscal Year: 2006
  3. DEVELOPMENT OF A PET RADIOTRACER FOR SIGMA-1 RECEPTOR
    Rikki Waterhouse; Fiscal Year: 2002
  4. Obesity is a Surgical Problem
    Ira Gantz; Fiscal Year: 2003
  5. MELANOCORTINS AND THE MC4R AND OBESITY
    Ira Gantz; Fiscal Year: 2002

Detail Information

Publications62

  1. doi Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments
    Joseph M Metzger
    Departments of Pharmacology, Rahway, NJ 07065, USA
    Am J Physiol Endocrinol Metab 299:E816-24. 2010
    ..The T(b) assay is a robust, information-rich assay that is simpler and has a greater throughput than measuring metabolic rate and is a practical, effective tool for drug discovery...
  2. ncbi Assessment of female and male fertility in Sprague-Dawley rats administered vorinostat, a histone deacetylase inhibitor
    L David Wise
    Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Birth Defects Res B Dev Reprod Toxicol 83:19-26. 2008
    ..These compounds are now marketed or are in clinical development. One such HDAC inhibitor, vorinostat (suberoylanilide hydroxamic acid [SAHA], Zolinza), was assessed for its potential effects on fertility in Sprague-Dawley rats...
  3. ncbi Mini review on molecular modeling of P-glycoprotein (Pgp)
    Sookhee N Ha
    Basic Chemistry, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Curr Top Med Chem 7:1525-9. 2007
    ..We review the recent developments from the point of view of methodology...
  4. ncbi Application of PCR technology in vaccine product development
    Jayanthi J Wolf
    Merck Research Laboratories, Biologics Safety Assessment, Merck and Co, Inc, PO Box 4, WP45 338, West Point, PA 19486, USA
    Expert Rev Vaccines 6:547-58. 2007
    ..The future outlook and the advantages and disadvantages of this technology are also discussed...
  5. ncbi Highly selective cascade couplings for the syntheses of functionalized piperidinones and bispidines
    Feng Xu
    Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA
    Org Lett 9:2669-72. 2007
    ..In addition, the cis isomer of 1 can be selectively obtained under acidic conditions, while the preparation of the corresponding trans isomer can also be readily realized through a base-catalyzed, dynamic crystallization-driven process...
  6. ncbi Isolation and structure of platencin: a FabH and FabF dual inhibitor with potent broad-spectrum antibiotic activity
    Hiranthi Jayasuriya
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
    Angew Chem Int Ed Engl 46:4684-8. 2007
  7. ncbi A practical synthesis of a gamma-secretase inhibitor
    Jeremy P Scott
    Department of Process Research, Merck Sharp and Dohme Research Laboratories, Hertford Road, Hoddesdon, Hertfordshire EN11 9BU, U K
    J Org Chem 72:4149-55. 2007
    ..The common cyclohexanone intermediate 5 was constructed by a regioselective Diels-Alder condensation of a 1,1-disubstituted vinyl sulfone 6 with 2-trimethylsiloxybutadiene...
  8. pmc Establishing acceptance criteria for cell-mediated-immunity assays using frozen peripheral blood mononuclear cells stored under optimal and suboptimal conditions
    Jeffrey G Smith
    Vaccine and Biologics Research, Merck Research Laboratories, WP26B 1144, Merck and Co, Inc, 770 Sumneytown Pike, West Point, PA 19486, USA
    Clin Vaccine Immunol 14:527-37. 2007
    ..Although all three AC measures could be effectively applied, the apoptosis AC limit applied was best for separating samples that could respond to antigenic stimulation from samples that could not effectively respond...
  9. ncbi One-step synthesis of alpha-chloro acetophenones from acid chlorides and aryl precursors
    Jonathan Rosen
    Merck and Company, Inc, Department of Process Research, P O Box 2000, Rahway, New Jersey 07065, USA
    Org Lett 9:667-9. 2007
    ..This method has significant generality and affords access to substitution patterns on aryl rings not directly achievable by Friedel-Crafts chemistry. [reaction: see text]...
  10. ncbi A generally applicable method for assessing the electrophilicity and reactivity of diverse nitrile-containing compounds
    Renata M Oballa
    Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Highway, Kirkland, Que, Canada H9H 3L1
    Bioorg Med Chem Lett 17:998-1002. 2007
    ..Moreover, there is a tentative link between high reactivity with cysteine and the potential to lead to irreversible covalent binding to proteins...
  11. ncbi p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold
    Swaminathan R Natarajan
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:5468-71. 2006
    ..Compound 16 reduced inflammation in animal disease models at EC(50) doses as low as 0.2mpk...
  12. ncbi Comparison between two classes of selective EP(3) antagonists and their biological activities
    Michel Belley
    Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire Dorval, Que, Canada H9R 4P8
    Bioorg Med Chem Lett 16:5639-42. 2006
    ..Some of those compounds, including hybrids containing the best structural features of both series, possess K(i) as low as 0.6 nM on the EP(3) receptor...
  13. ncbi Effect of cytochromes P450 chemical inhibitors and monoclonal antibodies on human liver microsomal esterase activity
    Stacey L Polsky-Fisher
    M S, Department of Drug Metabolism, WP75B 200, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:1361-6. 2006
    ..Additional experiments to assess the contribution of oxidative enzymes in the metabolism of esters may include incubations in the presence and absence of beta-nicotinamide adenine dinucleotide 2'-phosphate reduced...
  14. ncbi Evaluation of a potential stress effect in rat adjuvant arthritis by using a new and efficient plethysmograph
    Cordelia G Rasa
    Merck and Co, Rahway, NJ, USA
    J Am Assoc Lab Anim Sci 45:45-50. 2006
    ..Therefore, we do not recommend housing more than 4 rats per cage under these conditions...
  15. doi High-speed solubility screening assay using ultra-performance liquid chromatography/mass spectrometry in drug discovery
    Taro Yamashita
    Tsukuba Research Institute, Banyu Pharmaceutical Co Ltd, 3 Okubo, Tsukuba, Ibaraki 300 2611, Japan
    J Chromatogr A 1182:72-6. 2008
    ..Results obtained by the UPLC/MS and HPLC/UV systems showed good agreement, validating the usefulness of the UPLC/MS system. A high-speed solubility assay system was developed employing the UPLC/MS system, thereby tripling the throughput...
  16. doi A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies
    Zhizhen Zeng
    Imaging, Merck Research Laboratories, West Point, PA 19486, USA
    Nucl Med Biol 35:315-25. 2008
    ....
  17. doi Efficacy and safety of ezetimibe 40 mg vs. ezetimibe 10 mg in the treatment of patients with homozygous sitosterolaemia
    T Musliner
    Merck Research Laboratories, Rahway, NJ, USA
    Int J Clin Pract 62:995-1000. 2008
    ..To assess the effect of ezetimibe (EZE) 40 mg/day on non-cholesterol sterol plasma concentrations in patients with homozygous sitosterolaemia (HoS)...
  18. doi Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity
    Shuwen He
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:4399-405. 2010
    ..Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models...
  19. pmc Development of a population pharmacokinetic model for taranabant, a cannibinoid-1 receptor inverse agonist
    Xiujiang Susie Li
    Merck and Co, Inc, Whitehouse Station, New Jersey, USA
    AAPS J 12:537-47. 2010
    ..The pharmacokinetic profile of taranabant can adequately be described by a three-compartment model with first-order absorption and elimination. Clinical dose adjustment based on covariates effects is not warranted...
  20. doi A case study: lessons learned from human papillomavirus vaccine development: approval of a vaccine for use in children and young adolescents for prevention of an adult disease
    Elizabeth I O Garner
    Vaccines Clinical Research, Merck, Inc, North Wales, PA 19454, USA
    J Acquir Immune Defic Syndr 54:S50-2. 2010
    ....
  21. doi Patient-reported outcomes in a survey of patients treated with oral antihyperglycaemic medications: associations with hypoglycaemia and weight gain
    E Marrett
    Global Outcomes Research, Merck and Co, Inc, Whitehouse Station, NJ 08889, USA
    Diabetes Obes Metab 11:1138-44. 2009
    ..To examine the association between medication side-effects (SEs) and patient-reported outcomes (PROs) among patients with type 2 diabetes treated with oral antihyperglycaemic agents (OAHAs)...
  22. doi Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
    Andre Giroux
    Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Que, Canada H9H 3L1
    Bioorg Med Chem Lett 19:5837-41. 2009
    ..Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development...
  23. doi Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia
    Mark E Fraley
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 2, West Point, PA 19486, USA
    Expert Opin Ther Pat 19:1259-75. 2009
    ..Allosteric mGluR2 potentiators may offer advantages over orthosteric mGluR2/3 agonists as a result of their unique mode of action and ability to achieve superior mGluR2 selectivity...
  24. doi Hydrophilic interaction chromatography/tandem mass spectrometry for the simultaneous determination of three polar non-structurally related compounds, imipenem, cilastatin and an investigational beta-lactamase inhibitor, MK-4698, in biological matrices
    Yang Xu
    Merck Research Laboratories, Department of Drug Metabolism and Pharmacokinetics, 770 Sumneytown Pike, WP75B 300, West Point, PA 19486, USA
    Rapid Commun Mass Spectrom 23:2195-205. 2009
    ..This technique allowed rapid analysis of polar compounds in biologic matrixes with satisfactory chromatographic retention and increased throughput...
  25. doi Lipid-modifying efficacy and tolerability of extended-release niacin/laropiprant in patients with primary hypercholesterolaemia or mixed dyslipidaemia
    D Maccubbin
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Int J Clin Pract 62:1959-70. 2008
    ..Laropiprant (LRPT), a PGD(2) receptor (DP1) antagonist that reduces niacin-induced flushing has been combined with extended-release niacin (ERN) into a fixed-dose tablet...
  26. doi Efficacy of ezetimibe/simvastatin 10/40 mg compared to doubling the dose of low-, medium- and high-potency statin monotherapy in patients with a recent coronary event
    P Brudi
    Merck Schering Plough, New Jersey, NJ, USA
    Cardiology 113:89-97. 2009
    ..The aim of the study was to compare the efficacy/safety of doubling the dose of low-, medium- and high-potency statins on lipids/lipoproteins versus ezetimibe/simvastatin (EZE/SIMVA) 10/40 mg in patients with a recent coronary event...
  27. doi Potent benzimidazolone-based CGRP receptor antagonists
    Cory R Theberge
    Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 18:6122-5. 2008
    ..Blockade of CGRP-mediated vasodilation was observed with these compounds in a rhesus pharmacodynamic assay and the in vivo potency correlated with the in vitro activity in the serum-shifted functional assay...
  28. doi Optimization of a series of potent and selective ketone histone deacetylase inhibitors
    Giovanna Pescatore
    IRBM Merck Research Laboratories, Via Pontina Km 30, 600, 00040 Pomezia, Italy
    Bioorg Med Chem Lett 18:5528-32. 2008
    ..Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK...
  29. doi Double-blind active-control trials: beware the comparator you keep
    Mark J DiNubile
    Merck Research Laboratories, West Point, Pennsylvania, USA
    Clin Infect Dis 47:1064-7. 2008
    ..In phase II/III blinded, active-control trials, the reporting of adverse experiences attributed to a first-in-class drug might be confounded to a variable degree by expectations regarding a well-known comparator...
  30. doi Clinical course in migraine: conceptualizing migraine transformation
    Marcelo E Bigal
    Department of Neurology, Albert Einstein College of Medicine, Bronx, NY, USA
    Neurology 71:848-55. 2008
    ..Herein we discuss the evidence that migraine may transform and then consider potential mechanisms as well as risk factors. We close with a brief discussion of clinical strategies that arise based on this perspective on migraine...
  31. ncbi Different roles of liver X receptor alpha and beta in lipid metabolism: effects of an alpha-selective and a dual agonist in mice deficient in each subtype
    Erik G Lund
    Department of Cardiovascular Diseases, Merck Research Laboratories, Merck and Co, Inc, RY80W 250, P O Box 2000, Rahway, NJ 07065, United States
    Biochem Pharmacol 71:453-63. 2006
    ..Our data lend further experimental support to the hypothesis that LXRbeta-selective agonists may raise HDL-cholesterol and stimulate macrophage cholesterol efflux without causing liver triglyceride accumulation...
  32. ncbi Synthesis of benzo[b]furans via CuI-catalyzed ring closure
    Cheng yi Chen
    Department of Process Research, Merck and Co Inc, P O Box 2000, Rahway, NJ 07065, USA
    J Org Chem 70:6964-7. 2005
    ..A wide variety of benzo[b]furans were synthesized efficiently via a CuI-catalyzed ring closure of 2-haloaromatic ketones. The methodology was tolerant to various functional groups, affording benzofurans in 72-99% yields...
  33. ncbi Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1
    S L Colletti
    Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 11:107-11. 2001
    ..The conversion of apicidin, a nanomolar inhibitor of HDACs, into a series of side-chain analogues that display picomolar enzyme affinity is described within this structure-activity study...
  34. ncbi Chronic therapy with an ET(A/B) receptor antagonist in conscious dogs during progression of congestive heart failure. Intracellular Ca(2+) regulation and nitric oxide mediated coronary relaxation
    Y T Shen
    Department of Pharmacology, Merck Research Laboratories, WP46 200, 19486, West Point, PA, USA
    Cardiovasc Res 48:332-45. 2000
    ....
  35. ncbi Conserved cytoplasmic motifs that distinguish sub-groups of the polyprenol phosphate:N-acetylhexosamine-1-phosphate transferase family
    M S Anderson
    Department of Chemistry, State University of New York College of Environmental Science and Forestry, Syracuse, NY 13210, USA
    FEMS Microbiol Lett 191:169-75. 2000
    ..Four diverse loops are apparent, for MraY, WecA, WbcO and RgpG, that uniquely characterize these sub-groups of the transferase family, and a correlation is evident with the known or implied UDP-sugar specificity...
  36. ncbi Determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine using high-performance liquid chromatography with fluorescence detection
    M J Rose
    Merck Research Laboratories, Department of Drug Metabolism, West Point, PA 19486, USA
    J Chromatogr B Biomed Sci Appl 732:425-35. 1999
    ..Bovine serum albumin (0.5%) was used as an additive to urine to prevent precipitation of L-756 423 during the storage of clinical samples. The assay was used in support of human clinical trials...
  37. ncbi Determination of the viscosity of an amorphous drug using thermomechanical analysis (TMA)
    B C Hancock
    Merck Frosst Canada, Inc, Kirkland, Quebec
    Pharm Res 16:672-5. 1999
    ..This property of amorphous drugs and excipients is related to their average rate of molecular mobility and thus to their physical and chemical stability...
  38. pmc In vitro activities of the potent, broad-spectrum carbapenem MK-0826 (L-749,345) against broad-spectrum beta-lactamase-and extended-spectrum beta-lactamase-producing Klebsiella pneumoniae and Escherichia coli clinical isolates
    J Kohler
    Departments of Infectious Diseases, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    Antimicrob Agents Chemother 43:1170-6. 1999
    ..Importantly, MK-0826 MICs remained at or below 1 microgram/ml under all test conditions...
  39. ncbi Use of a phosphotyrosine-antibody pair as a general detection method in homogeneous time-resolved fluorescence: application to human immunodeficiency viral protease
    R T Cummings
    Department of Molecular Design and Diversity, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    Anal Biochem 269:79-93. 1999
    ..4 +/- 2.7 nM for the HIV protease monomer-dimer equilibrium. The HTRF assay was also utilized to measure the inhibition of the enzyme by two known inhibitors...
  40. ncbi Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase
    R B Lingham
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, and Merck Research Laboratories, Sumneytown Pike, West Point, Pennsylvania 19486, USA
    J Med Chem 41:4492-501. 1998
    ..04 --> 100 microM) against FPTase. Modest changes in the structures of these inhibitors dramatically change the inhibitory activity of these inhibitors...
  41. ncbi Metabolite-P450 complex formation by methylenedioxyphenyl HIV protease inhibitors in rat and human liver microsomes
    M Chiba
    Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
    Biochem Pharmacol 56:223-30. 1998
    ....
  42. ncbi Photoaffinity labeling of the benzodiazepine binding site of alpha1beta3gamma2 gamma-aminobutyric acidA receptors with flunitrazepam identifies a subset of ligands that interact directly with His102 of the alpha subunit and predicts orientation of these w
    R M McKernan
    Department of Biochemistry, Merck Sharp and Dohme Research Laboratories, Harlow, Essex, UK CM2O 2QR
    Mol Pharmacol 54:33-43. 1998
    ..The data in the current study indicate that His102 interacts directly with the pendant phenyl group of diazepam, and further implications for the pharmacophore of the BZ binding site are discussed...
  43. ncbi Kinetic mechanism of glutathione conjugation to leukotriene A4 by leukotriene C4 synthase
    N Gupta
    Department of Pharmacology and Therapeutics, McGill University, 3655 Drummond, Montreal, Quebec, Canada
    Biochim Biophys Acta 1391:157-68. 1998
    ..The rate equation for the random equilibrium mechanism accommodates the inhibition patterns observed for L-699,333 against both substrates as revealed by kinetic fits of the inhibition data to the overall rate equation...
  44. ncbi A combinatorial approach defines specificities of members of the caspase family and granzyme B. Functional relationships established for key mediators of apoptosis
    N A Thornberry
    Department of Enzymology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Biol Chem 272:17907-11. 1997
    ....
  45. ncbi Functional characterization of human gamma-aminobutyric acidA receptors containing the alpha 4 subunit
    K A Wafford
    Merck Sharp and Dohme Research Laboratories, Harlow, Essex, UK
    Mol Pharmacol 50:670-8. 1996
    ..These experiments reveal a unique pharmacology for alpha 4-containing receptors with some similarities to both alpha 6- and alpha 1-containing receptors...
  46. ncbi Effect of alendronate and MK-677 (a growth hormone secretagogue), individually and in combination, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women
    M G Murphy
    Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    J Clin Endocrinol Metab 86:1116-25. 2001
    ....
  47. ncbi A-fibres sprouting from lamina I into lamina II of spinal dorsal horn after peripheral nerve injury in rats
    Q P Ma
    Department of Anatomy and Developmental Biology, University College London, Gower Street, WC1E 6BT, London, UK
    Brain Res 904:137-40. 2001
    ..This result suggests that A-fibre sprouting arise after peripheral nerve injury, but mainly from small calibre Adelta-fibres which terminate in lamina I...
  48. ncbi 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I
    Jason M Elliott
    Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    Bioorg Med Chem Lett 12:1755-8. 2002
    ....
  49. ncbi Embracing complexity, inching closer to reality
    Eric E Schadt
    Rosetta Inpharmatics, 401 Terry Avenue North, Seattle, WA 98109, USA
    Sci STKE 2005:pe40. 2005
    ....
  50. ncbi Bridging cheminformatic metabolite prediction and tandem mass spectrometry
    M Reza Anari
    Department of Drug Metabolism, Merck Research LaboratoriesWP75A 203, Sumneytown Pike, West Point, PA 19486, USA
    Drug Discov Today 10:711-7. 2005
    ..The following discussion highlights the significance of knowledge of the metabolite mass in facilitating the detection and structural elucidation of drug metabolites...
  51. ncbi Subcellular targeting of DISC1 is dependent on a domain independent from the Nudel binding site
    N J Brandon
    Merck Sharp and Dohme Research Labs, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK
    Mol Cell Neurosci 28:613-24. 2005
    ....
  52. ncbi An efficient synthesis of an alphavbeta3 antagonist
    Nobuyoshi Yasuda
    Department of Process Research, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    J Org Chem 69:1959-66. 2004
    ..The central imidazolidone portion was created from these two components using an effective three-step cyclization protocol. Thus, a highly convergent process for the drug candidate was defined...
  53. ncbi State-dependent inhibition of L-type calcium channels: cell-based assay in high-throughput format
    Menghang Xia
    Department of Molecular Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA
    Anal Biochem 327:74-81. 2004
    ..Overall, this novel assay can be used to identify state-dependent calcium channel antagonists and should be useful for evaluating state-dependent inhibitory potency of a large number of samples...
  54. ncbi Characterization of lysophosphatidic acid and sphingosine-1-phosphate-mediated signal transduction in rat cortical oligodendrocytes
    Naichen Yu
    Molecular Neuroscience, Merck Research Laboratories, San Diego, California 92121, USA
    Glia 45:17-27. 2004
    ..These results taken together suggest that lysophospholipid receptor activation involves receptor coupling to heterotrimeric Gq subunits with consequent activation of PLC, PKC, and MAPK pathways leading to ERK phosphorylation...
  55. ncbi Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype
    Feroze Ujjainwalla
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 13:4431-5. 2003
    ..The discovery and optimization of a new class of non-peptidyl, pyridazinone derived melanocortin subtype-4 receptor agonists is disclosed...
  56. ncbi Structural analysis of oligosaccharides by a combination of electrospray mass spectrometry and bromine isotope tagging of reducing-end sugars with 2-amino-5-bromopyridine
    Min Li
    Regulatory and Analytical Sciences Analytical, Merck and Co, Inc, WP82 30, P O Box 4, West Point, PA 19486, USA
    Rapid Commun Mass Spectrom 17:1462-6. 2003
    ..No fragment ions arising from loss of the bromine atom were observed...
  57. ncbi Proving non-inferiority or equivalence of two treatments with dichotomous endpoints using exact methods
    I S F Chan
    Clinical Biostatistics, Merck Research Laboratories, West Point, PA 19486, USA
    Stat Methods Med Res 12:37-58. 2003
    ..Finally, we illustrate with several examples the application of these exact methods in analysing and planning non-inferiority or equivalence trials...
  58. ncbi Asthma control and patient satisfaction among early pediatric users of montelukast
    Siva Narayanan
    Outcomes Research and Management, Merck and Co, Inc, West Point, Pennsylvania 19486, USA
    J Asthma 39:757-65. 2002
    ..To assess asthma control and patient satisfaction among pediatric users of montelukast in a clinical practice setting...
  59. ncbi Analysing mice. Commentary on Stephens et al. 'Studying the neurobiology of stimulant and alcohol abuse and dependence in genetically manipulated mice'
    N M J Rupniak
    Department of Behavioural Neuroscience, Marck Sharp and Dohme Neuroscience Research Center, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    Behav Pharmacol 13:353-4. 2002
  60. ncbi N-aryl-prolyl-dipeptides as potent antagonists of VLA-4
    Theodore M Kamenecka
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 12:2205-8. 2002
    ..Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues...
  61. ncbi Activation of spinal group I metabotropic glutamate receptors in rats evokes local glutamate release and spontaneous nociceptive behaviors: effects of 2-methyl-6-(phenylethynyl)-pyridine pretreatment
    Daniel S Lorrain
    Department of Neuropharmacology, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Neurosci Lett 327:198-202. 2002
    ..These results suggest that stimulation of spinal mGluR5 leads to glutamate release within the spinal cord, a response that may in part account for the nociceptive behaviors evoked by i.t. (S)-3,5-DHPG...
  62. ncbi Transgenic mice with muscle-specific insulin resistance develop increased adiposity, impaired glucose tolerance, and dyslipidemia
    D E Moller
    Department of Medicine, Beth Israel Hospital, Boston, Massachusetts, USA
    Endocrinology 137:2397-405. 1996
    ....

Research Grants12

  1. Keystone Symposium: Eicosanoid Lipid Mediators
    Jilly Evans; Fiscal Year: 2003
    ..NIH support for this meeting will allow more graduate student and postdoctoral participation in.this exciting multidisciplinary meeting. ..
  2. The Molecular and Integrative Basis for Toxic Responses
    Roger Ulrich; Fiscal Year: 2006
    ....
  3. DEVELOPMENT OF A PET RADIOTRACER FOR SIGMA-1 RECEPTOR
    Rikki Waterhouse; Fiscal Year: 2002
    ....
  4. Obesity is a Surgical Problem
    Ira Gantz; Fiscal Year: 2003
    ..This will involve the use of neuroanatomical techniques and in vivo physiological experiments. The intent of Specific Aims 3 and 4 is to expand understanding of the complex process of energy homeostasis. ..
  5. MELANOCORTINS AND THE MC4R AND OBESITY
    Ira Gantz; Fiscal Year: 2002
    ..Finally, we propose to examine the mechanisms through which AGRP antagonizes the melanocortins by characterizing the action of recombinant AGRP. ..