期刊
SYNAPSE
卷 66, 期 10, 页码 880-884出版社
WILEY
DOI: 10.1002/syn.21579
关键词
5-HT1A; [11C]CUMI-101; citalopram; human; PET
资金
- Lundbeck Foundation
- Danish Council for Independent Research I Humanities
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-HT1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273277; Kumar et al. [2006] J Med Chem 49:125134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243249). 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. (c) 2012 Wiley Periodicals, Inc.
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