6533b853fe1ef96bd12ad555
RESEARCH PRODUCT
Ex vivo and in vivo evaluation of [18F]PR04.MZ in rodents: a selective dopamine transporter imaging agent.
Patrick J. RissFrank RoeschUlrich SchmidtHartmut LueddensFabian DebusPatrick SchlossRené Hummerichsubject
MaleFluorine RadioisotopesDopamine Plasma Membrane Transport ProteinsBiochemistryCell LineRats Sprague-DawleyIn vivoDrug DiscoveryAnimalsHumansTissue DistributionGeneral Pharmacology Toxicology and PharmaceuticsSerotonin transporterDopamine transporterPharmacologySerotonin Plasma Membrane Transport ProteinsDopamine Plasma Membrane Transport ProteinsNorepinephrine Plasma Membrane Transport ProteinsbiologyChemistryOrganic ChemistryTransporterLigand (biochemistry)Imaging agentRatsBiochemistryPositron-Emission Tomographybiology.proteinBiophysicsMolecular MedicineRadiopharmaceuticalsEx vivoTropanesdescription
N-4-Fluorobut-2-yn-1-yl-2beta-carbomethoxy-3beta-phenyltropane (PR04.MZ) has been developed as dopamine transporter (DAT) ligand for molecular imaging. It contains a terminally fluorinated, conformationally constrained nitrogen substituent that is well suited for the introduction of fluorine-18. The present report describes the pharmacological characterisation of [18F]PR04.MZ. The ligand shows an IC50 value of 2 nM against human DAT, whereas the IC50 value against human serotonin transporter and human noradrenalin transporter are lower (110 nM and 22 nM, respectively). Furthermore, its ex vivo organ distribution, its binding profile in the rat brain and reversibility of binding were examined. A muPET study illuminates a fast kinetic profile and specific binding to rat DAT.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2009-09-04 | ChemMedChem |