No change in [ 11C]CUMI-101 binding to 5-HT 1A receptors after intravenous citalopram in human

Lars H. Pinborg*, Ling Feng, Mette E. Haahr, Nic Gillings, Agnete Dyssegaard, Jacob Madsen, Claus Svarer, Stig Yndgaard, Troels W. Kjaer, Ramin V. Parsey, Hanne D. Hansen, Anders Ettrup, Olaf B. Paulson, Gitte M. Knudsen

*Corresponding author af dette arbejde

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    Abstrakt

    The main objective of this study was to determine the sensitivity of [ 11C]CUMI-101 to citalopram challenge aiming at increasing extracellular 5-HT. CUMI-101 has agonistic properties in human embryonic kidney 293 cells transfected with human recombinant 5-HT 1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273-277; Kumar et al. [2006] J Med Chem 49:125-134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243-249). We studied six healthy individuals. Two PET-scans were performed on the same day in each individual before and after constant infusion of citalopram (0.15 mg/kg). The imaging data were analyzed using two tissue compartment kinetic modeling with metabolite corrected arterial input and Simplified Reference Tissue Modeling using cerebellum as a reference region. There was no significant difference in regional distribution volume or non-displaceable binding potential values before and after citalopram infusion. The mean receptor occupancy was 0.03 (range -0.14 to 0.17). Our data imply that [ 11C]CUMI-101 binding is not sensitive to citalopram infusion in humans. Synapse, 2012.

    OriginalsprogEngelsk
    Sider (fra-til)880-884
    Antal sider5
    TidsskriftSynapse
    Vol/bind66
    Udgave nummer10
    DOI
    StatusUdgivet - 1 okt. 2012

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