Joseph M Metzger

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. doi request reprint 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. doi request reprint Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
    Jian Liu
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2074-7. 2010
  3. doi request reprint Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity
    Xiao Ming Guan
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Cell Metab 11:101-12. 2010
  4. doi request reprint Reduced sensitivity to diet-induced obesity in mice carrying a mutant 5-HT6 receptor
    Andrea Frassetto
    Department of Metabolic Disorders, Merck Research Laboratories, P O Box 2000, RY80M 213, Rahway, NJ 07065, USA
    Brain Res 1236:140-4. 2008
  5. doi request reprint Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist
    Xiao Ming Guan
    Department of Metabolic Disorders, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    J Pharmacol Exp Ther 336:356-64. 2011
  6. ncbi request reprint Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents
    Lauren P Shearman
    Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065, United States
    Eur J Pharmacol 579:215-24. 2008
  7. doi request reprint Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands
    Qingmei Hong
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 20:4483-6. 2010
  8. doi request reprint Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species
    Yue Feng
    Department of Diabetes and Obesity, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:4106-15. 2011
  9. doi request reprint Effects of peripherally administered neuromedin U on energy and glucose homeostasis
    Andrea M Peier
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:2644-54. 2011
  10. pmc FGF21 analogs of sustained action enabled by orthogonal biosynthesis demonstrate enhanced antidiabetic pharmacology in rodents
    James Mu
    Department of Metabolic Disease Diabetes, Merck Research Laboratories, Rahway, New Jersey, USA
    Diabetes 61:505-12. 2012

Collaborators

Detail Information

Publications15

  1. doi request reprint 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. doi request reprint Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
    Jian Liu
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2074-7. 2010
    ..After oral administration, compound 9 had sufficient exposure in diet induced obese mice to demonstrate efficacy in lowering food intake and body weight via BRS-3 activation...
  3. doi request reprint Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity
    Xiao Ming Guan
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Cell Metab 11:101-12. 2010
    ..These results demonstrate that BRS-3 has a role in energy homeostasis that complements several well-known pathways and that BRS-3 agonists represent a potential approach to the treatment of obesity...
  4. doi request reprint Reduced sensitivity to diet-induced obesity in mice carrying a mutant 5-HT6 receptor
    Andrea Frassetto
    Department of Metabolic Disorders, Merck Research Laboratories, P O Box 2000, RY80M 213, Rahway, NJ 07065, USA
    Brain Res 1236:140-4. 2008
    ..Given the documented role of the serotonin systems in human feeding, our results provide an interesting piece of evidence supporting the development of 5-HT6 receptor antagonists for treating obesity...
  5. doi request reprint Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist
    Xiao Ming Guan
    Department of Metabolic Disorders, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    J Pharmacol Exp Ther 336:356-64. 2011
    ..Our results demonstrate antiobesity efficacy for MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity...
  6. ncbi request reprint Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents
    Lauren P Shearman
    Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065, United States
    Eur J Pharmacol 579:215-24. 2008
    ..These findings suggest that selective cannabinoid CB(1) receptor inverse agonists such as Imidazole 24b have potential for the treatment of obesity...
  7. doi request reprint Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands
    Qingmei Hong
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 20:4483-6. 2010
    ..The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties...
  8. doi request reprint Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species
    Yue Feng
    Department of Diabetes and Obesity, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:4106-15. 2011
    ..Thus, in addition to its potential role in the treatment of obesity, BRS-3 may also regulate blood glucose levels and have a role in the treatment of diabetes mellitus...
  9. doi request reprint Effects of peripherally administered neuromedin U on energy and glucose homeostasis
    Andrea M Peier
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:2644-54. 2011
    ..Collectively, these data suggest that NMU functions as a peripheral regulator of energy and glucose homeostasis and the development of NMUR1 agonists may be an effective treatment for diabetes and obesity...
  10. pmc FGF21 analogs of sustained action enabled by orthogonal biosynthesis demonstrate enhanced antidiabetic pharmacology in rodents
    James Mu
    Department of Metabolic Disease Diabetes, Merck Research Laboratories, Rahway, New Jersey, USA
    Diabetes 61:505-12. 2012
    ..PEGylation of human FGF21 at a specific and preferred site confers superior metabolic pharmacology...
  11. pmc Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism
    Donald J Marsh
    Department of Obesity Research, Animal Pharmacology, and Comparative Medicine, Merck Research Laboratories, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 99:3240-5. 2002
    ..We conclude that MCH1R is a physiologically relevant MCH receptor in mice that plays a role in energy homeostasis through multiple actions on locomotor activity, metabolism, appetite, and neuroendocrine function...
  12. ncbi request reprint The mu-opioid receptor subtype is required for the anorectic effect of an opioid receptor antagonist
    Jiaping Zhang
    Department of Metabolic Disorders, Merck Research Laboratories, P O Box 2000, RY80M 213, Rahway, NJ 07065, USA
    Eur J Pharmacol 545:147-52. 2006
    ..Our results suggest an important role for the mu-opioid receptor subtype in animal feeding regulation and support the development of mu-selective antagonists as potential agents for treating human obesity...
  13. doi request reprint The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization
    Harry R Chobanian
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem 20:2845-9. 2012
    ..This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature...
  14. doi request reprint Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists
    Shuwen He
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:1913-7. 2010
    ..This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3...
  15. pmc 11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice
    Anne Hermanowski-Vosatka
    Merck Research Laboratories, Merck and Company, Rahway, NJ 07065, USA
    J Exp Med 202:517-27. 2005
    ....