PETER MELTZER

Summary

Affiliation: Organix Inc
Country: USA

Publications

  1. ncbi request reprint Design and synthesis of an irreversible dopamine-sparing cocaine antagonist
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 10:3583-91. 2002
  2. ncbi request reprint 3-Aryl-2-carbomethoxybicyclo[3.2.1]oct-2-enes inhibit WIN 35,428 binding potently and selectively at the dopamine transporter
    P C Meltzer
    Organix Inc, Woburn, MA 01801, USA
    Bioorg Med Chem 8:581-90. 2000
  3. pmc 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 49:1420-32. 2006
  4. pmc The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 16:1832-41. 2008
  5. ncbi request reprint Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem Lett 13:4133-7. 2003
  6. ncbi request reprint A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    J Med Chem 46:3483-96. 2003
  7. ncbi request reprint Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 46:1538-45. 2003
  8. ncbi request reprint Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters
    P C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 44:2619-35. 2001
  9. ncbi request reprint 2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters
    P C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 43:2982-91. 2000
  10. pmc Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters
    Duy Phong Pham-Huu
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 15:1067-82. 2007

Research Grants

Detail Information

Publications14

  1. ncbi request reprint Design and synthesis of an irreversible dopamine-sparing cocaine antagonist
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 10:3583-91. 2002
    ..In contrast, the epoxide 7 showed a greater inhibition of dopamine reuptake than cocaine binding at 24h (68% versus 18%)...
  2. ncbi request reprint 3-Aryl-2-carbomethoxybicyclo[3.2.1]oct-2-enes inhibit WIN 35,428 binding potently and selectively at the dopamine transporter
    P C Meltzer
    Organix Inc, Woburn, MA 01801, USA
    Bioorg Med Chem 8:581-90. 2000
    ..2.1]octane system affects the interaction of these molecules with the serotonin transporter far more markedly than it affects the interaction with the dopamine transporter...
  3. pmc 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 49:1420-32. 2006
    ..Among the most potent of these DAT/NET selective compounds are the 1-(3,4-dichlorophenyl)- (4u) and the 1-naphthyl- (4t) 2-pyrrolidin-1-yl-pentan-1-one analogues...
  4. pmc The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 16:1832-41. 2008
    ..We conclude that it is unlikely that there exist two tropane binding sites in close proximity to one another on either the DAT or SERT...
  5. ncbi request reprint Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem Lett 13:4133-7. 2003
    ..Compound 10, a diacetoxy prodrug for 7, substituted fully for cocaine in a rat drug-discrimination paradigm and is now undergoing further investigation as a potential medication for cocaine abuse...
  6. ncbi request reprint A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    J Med Chem 46:3483-96. 2003
    ..s...
  7. ncbi request reprint Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 46:1538-45. 2003
    ..The threo isomers are potent and selective inhibitors of the DAT. This is the first generalization of the principle that the presence of nitrogen is not a necessity for DAT inhibition...
  8. ncbi request reprint Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters
    P C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 44:2619-35. 2001
    ..The general SAR of the tropanes is maintained and the rank order of potencies based on substitution at the C3 position remains 3,4-dichloro > 2-naphthyl > 4-fluoro > phenyl...
  9. ncbi request reprint 2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters
    P C Meltzer
    Organix Inc, 240 Salem Street, Woburn, Massachusetts 01801, USA
    J Med Chem 43:2982-91. 2000
    ..2.1]octanes yields potent inhibitors of monoamine transport. Therefore neither nitrogen nor oxygen are prerequisites for binding of tropane-like ligands to monoamine transporters...
  10. pmc Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters
    Duy Phong Pham-Huu
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem 15:1067-82. 2007
    ..The (1R)-configuration provided the eutomers...
  11. ncbi request reprint Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters
    Peter C Meltzer
    Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
    Bioorg Med Chem Lett 14:6007-10. 2004
    ..The 3,4-dichlorophenyl-8-thiabicyclo[3.2.1]oct-2-ene (4f) is particularly potent (IC50=4.5 nM) and selective (800-fold) with respect to inhibition of the serotonin transporter...
  12. ncbi request reprint Non-amine-based dopamine transporter (reuptake) inhibitors retain properties of amine-based progenitors
    Bertha K Madras
    Department of Psychiatry, Harvard Medical School, New England Primate Research Center, 1 Pine Hill Drive, Southborough, MA 01772 9102, USA
    Eur J Pharmacol 479:41-51. 2003
    ..These novel drugs compel a revision of current concepts of drug-monoamine transporter complex formation and open avenues for discovery of a new generation of therapeutic drugs...
  13. ncbi request reprint Dopamine transporter (DAT) inhibitors alleviate specific parkinsonian deficits in monkeys: association with DAT occupancy in vivo
    Bertha K Madras
    Department of Psychiatry, Harvard Medical School, Division of Neurochemistry, New England Primate Research Center, 1 Pine Hill Dr, Southborough, MA 01772 9102, USA
    J Pharmacol Exp Ther 319:570-85. 2006
    ..The therapeutic potential of dopamine transport inhibitors for Parkinson's disease warrants preclinical investigation...
  14. pmc Further evidence of dopamine transporter dysregulation in ADHD: a controlled PET imaging study using altropane
    Thomas J Spencer
    Pediatric Psychopharmacology Unit, Psychiatry Service Massachusetts General Hospital, Boston, Massachusetts, USA
    Biol Psychiatry 62:1059-61. 2007
    ..The findings of in vivo neuroimaging of DAT in ADHD have been somewhat discrepant, however...

Research Grants10

  1. Discovery of Novel Pharmacotherapies: Cocaine Dependence
    PETER MELTZER; Fiscal Year: 2007
    ..vi) analogues of pyrovalerone. ..
  2. DISCOVERY OF NOVEL PHARMACOTHERAPIES--COCAINE DEPENDENCE
    PETER MELTZER; Fiscal Year: 2001
    ..It is anticipated that these studies will lead to a disclosure of SAR on aspects of the tropanes hitherto uninvestigated. ..