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Radiosynthesis and in vivo evaluation of a series of substituted C-phenethylamines as 5-HT2A agonist

Radiosynthesis and in vivo evaluation of a series of substituted C-phenethylamines as 5-HT2A agonist

  1. catseye
    Eur J Nucl Med Mol Imaging (2011) 38:681–693

    Anders Ettrup & Martin Hansen & Martin A. Santini & James Paine & Nic Gillings & Mikael Palner & Szabolcs Lehel & Matthias M. Herth & Jacob Madsen & Jesper Kristensen & Mikael Begtrup & Gitte M. Knudsen

    ABSTRACT:
    Purpose Positron emission tomography (PET) imaging of serotonin 2A (5-HT2A) receptors with agonist tracers holds promise for the selective labelling of 5-HT2A receptors in their high-affinity state. We have previously validated [11C]Cimbi-5
    and found that it is a 5-HT2A receptor agonist PET tracer. In an attempt to further optimize the target-to-background binding ratio, we modified the chemical structure of the phenethylamine
    backbone and carbon-11 labelling site of [11C]Cimbi-5 in different ways. Here, we present the in vivo validation of nine novel 5-HT2A receptor agonist PET tracers in the pig brain.