| Literature DB >> 19577467 |
Magnus Schou1, Carsten Steiger, Andrea Varrone, Denis Guilloteau, Christer Halldin.
Abstract
A new dopamine transporter (DAT) ligand, (E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4'-methyl-phenyl) nortropane (FE-PE2I, 6), derived from PE2I (1), was prepared and found to be a potent inhibitor of rodent DAT in vitro. Compound 6 was radiolabelled with fluorine-18 (t(1/2)=109.8 min) for PET studies in monkeys. In vivo PET measurements showed a regional distribution in brain that corresponds to the known distribution of DAT. This binding was specific, reversible and the kinetics of [(18)F]6 binding in brain were faster than for its lead compound, [(11)C]1. The possible presence of a hydroxymethyl-radiometabolite formed by oxidation in the 3beta-benzylic position of [(18)F]6 warrants further detailed evaluation of the metabolism of [(18)F]6. [(18)F]6 is a potential radioligand for imaging DATs in the human brain with PET.Entities:
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Year: 2009 PMID： 19577467 DOI： 10.1016/j.bmcl.2009.06.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823