Search results for "Monoamine transporter"

showing 2 items of 2 documents

The DAT ligand [(18)F]PR17.MZ mirrors the in vivo pharmacokinetic profile of [(11)C]cocaine with significantly improved monoamine transporter selecti…

2010

Fluorine RadioisotopesContrast MediaPharmacologyLigandsBiochemistryRats Sprague-DawleyPharmacokineticsCocaineIn vivoDrug DiscoverymedicineAnimalsBiogenic MonoaminesCarbon RadioisotopesGeneral Pharmacology Toxicology and PharmaceuticsDopamine transporterPharmacologyDopamine Plasma Membrane Transport ProteinsMonoamine transporterbiologymedicine.diagnostic_testChemistryOrganic ChemistryLigand (biochemistry)RatsBiochemistryPositron emission tomographyPositron-Emission Tomographybiology.proteinMolecular MedicineRadiopharmaceuticalsSelectivityChemMedChem
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Synthesis and monoamine uptake inhibition of conformationally constrained 2β-carbomethoxy-3β-phenyl tropanes

2009

A series of 2beta-carbomethoxy-3beta-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity.

StereochemistryMolecular ConformationLigandsBiochemistryStructure-Activity Relationshipchemistry.chemical_compoundHumansBiogenic MonoaminesPhysical and Theoretical ChemistrySerotonin transporterDopamine transporterSerotonin Plasma Membrane Transport ProteinsDopamine Plasma Membrane Transport ProteinsNorepinephrine Plasma Membrane Transport ProteinsbiologyMonoamine transporterChemistryOrganic ChemistryHEK 293 cellsBiological TransportStereoisomerismTransporterTropaneMonoamine neurotransmitterbiology.proteinSelectivityTropanesOrganic & Biomolecular Chemistry
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