Mark S Chambers

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Open-label, long-term safety study of cevimeline in the treatment of postirradiation xerostomia
    Mark S Chambers
    Department of Head and Neck Surgery, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Int J Radiat Oncol Biol Phys 69:1369-76. 2007
  2. ncbi request reprint 6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    J Med Chem 45:1176-9. 2002
  3. ncbi request reprint Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    J Med Chem 46:2227-40. 2003
  4. ncbi request reprint An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    J Med Chem 47:5829-32. 2004
  5. doi request reprint In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist
    John R Atack
    Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom
    J Pharmacol Exp Ther 331:470-84. 2009
  6. ncbi request reprint Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction
    Philip Jones
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    Bioorg Med Chem Lett 16:872-5. 2006
  7. ncbi request reprint 3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors
    Helen J Szekeres
    Merck, Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    Bioorg Med Chem Lett 14:2871-5. 2004
  8. ncbi request reprint Cevimeline for the treatment of postirradiation xerostomia in patients with head and neck cancer
    Mark S Chambers
    Department of Head and Neck Surgery, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    Int J Radiat Oncol Biol Phys 68:1102-9. 2007

Detail Information

Publications8

  1. ncbi request reprint Open-label, long-term safety study of cevimeline in the treatment of postirradiation xerostomia
    Mark S Chambers
    Department of Head and Neck Surgery, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Int J Radiat Oncol Biol Phys 69:1369-76. 2007
    ..To assess the safety of long-term cevimeline treatment of radiation-induced xerostomia in patients with head-and-neck cancer; and to assess the efficacy of cevimeline in these patients...
  2. ncbi request reprint 6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    J Med Chem 45:1176-9. 2002
    ..In particular, 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5H)-one (26) has been identified as a functionally selective GABA-A alpha5 inverse agonist...
  3. ncbi request reprint Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    J Med Chem 46:2227-40. 2003
    ....
  4. ncbi request reprint An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties
    Mark S Chambers
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    J Med Chem 47:5829-32. 2004
    ..It does not exhibit the convulsant, proconvulsant, or anxiogenic activity associated with nonselective GABA(A) inverse agonists...
  5. doi request reprint In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist
    John R Atack
    Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom
    J Pharmacol Exp Ther 331:470-84. 2009
    ..5 mg, which, along with its variable human pharmacokinetics, precluded its further development...
  6. ncbi request reprint Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction
    Philip Jones
    Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK
    Bioorg Med Chem Lett 16:872-5. 2006
    ..An unusual oxidation of the pyrazolo[1,5-d][1,2,4]triazine core to the corresponding pyrazolo[1,5-d][1,2,4]triazin-4(5H)-one scaffold by aldehyde oxidase has been observed...
  7. ncbi request reprint 3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors
    Helen J Szekeres
    Merck, Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
    Bioorg Med Chem Lett 14:2871-5. 2004
    ....
  8. ncbi request reprint Cevimeline for the treatment of postirradiation xerostomia in patients with head and neck cancer
    Mark S Chambers
    Department of Head and Neck Surgery, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    Int J Radiat Oncol Biol Phys 68:1102-9. 2007
    ..To study the efficacy and safety of cevimeline in two double-blind trials (Studies 003 and 004) enrolling patients with head and neck cancer in whom xerostomia developed after radiotherapy...