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    J Med Chem. 2008 Dec 25;51(24):7788-99.

    Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.

    Stehouwer JS, Jarkas N, Zeng F, Voll RJ, Williams L, Camp VM, Malveaux EJ, Votaw JR, Howell L, Owens MJ, Goodman MM.

    Source

    Department of Radiology, Emory University, Atlanta, GA, USA.

    Abstract

    The meta-vinylhalide fluoroalkyl ester nortropanes 1-4 were synthesized as ligands of the serotonin transporter (SERT) for use as positron emission tomography (PET) imaging agents. In vitro competition binding assays demonstrated that 1-4 have a high affinity for the SERT (K(i) values = 0.3-0.4 nM) and are selective for the SERT over the dopamine and norepinephrine transporters (DAT and NET). MicroPET imaging in anesthetized cynomolgus monkeys with [(18)F]1-[(18)F]4 demonstrated that all four tracers behave similarly with peak uptake in the SERT-rich brain regions achieved after 45-55 min, followed by a steady washout. An awake monkey study was performed with [(18)F]1, which demonstrated that the uptake of [(18)F]1 was not influenced by anesthesia. Chase studies with the SERT ligand 15 displaced [(18)F]1-[(18)F]4, but chase studies with the DAT ligand 16 did not displace [(18)F]1-[(18)F]4 thus indicating that the tracers were binding specifically to the SERT.

    PMID:
    19053782
    [PubMed - indexed for MEDLINE]
    PMCID:
    PMC2668213
    Free PMC Article

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