Research Topics
Genomes and GenesSpecies | PETER MELTZERSummaryAffiliation: Organix Inc Country: USA Publications
Research Grants
| Collaborators
|
Detail Information
Publications
Design and synthesis of an irreversible dopamine-sparing cocaine antagonistPeter 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%)...- 3-Aryl-2-carbomethoxybicyclo[3.2.1]oct-2-enes inhibit WIN 35,428 binding potently and selectively at the dopamine transporterP 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... - 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitorsPeter 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... - 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 transportersPeter 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... - Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanesPeter 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... - A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brainPeter C Meltzer
Organix Inc, 240 Salem Street, Woburn, MA 01801, USA
J Med Chem 46:3483-96. 2003..s... - Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidatePeter 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... - Synthesis of 6- and 7- hydroxy-8-azabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transportersP 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... - 2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transportersP 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... - Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transportersDuy 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... - Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transportersPeter 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... - Non-amine-based dopamine transporter (reuptake) inhibitors retain properties of amine-based progenitorsBertha 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... - Dopamine transporter (DAT) inhibitors alleviate specific parkinsonian deficits in monkeys: association with DAT occupancy in vivoBertha 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... - Further evidence of dopamine transporter dysregulation in ADHD: a controlled PET imaging study using altropaneThomas 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 Grants
- Discovery of Novel Pharmacotherapies: Cocaine DependencePETER MELTZER; Fiscal Year: 2007..vi) analogues of pyrovalerone. ..
- DISCOVERY OF NOVEL PHARMACOTHERAPIES--COCAINE DEPENDENCEPETER MELTZER; Fiscal Year: 2001..It is anticipated that these studies will lead to a disclosure of SAR on aspects of the tropanes hitherto uninvestigated. ..