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Analysis of 5-HT2A Receptor Binding with [C-11]MDL 100907 in Rats: Optimization of Kinetic Modeling

Visser, A. K. D., De Vries, E. F. J., K. Ramakrishnan, N., Willemsen, A. T. M., Bosker, F. J., den Boer, J. A., Dierckx, R. A. J. O. & van Waarde, A., Dec-2013, In : Molecular Imaging and Biology. 15, 6, p. 730-738 9 p.

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  • Visser2013

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Preclinical positron emission tomography studies are important to follow disease progression and develop new pharmacological agents. We investigated whether kinetic modeling of 5-HT2A tracer [C-11]MDL 100907 is possible in rats.

Kinetic modeling with either metabolite-corrected plasma curve or with the cerebellum as a reference tissue resulted in a good correlation of nondisplaceable binding potential (BPND) calculated from a two-tissue compartment model (2TCM) or different reference tissue models. Injecting the tracer by a slower bolus decreases the variation in 2TCM outcome parameters and results in a good correlation between k(3)/k(4) and the other models. Application of 0.2 mg/kg cold MDL 100907 resulted in almost complete occupancy of 5-HT2A receptors.

A reference tissue model can be used for [C-11]MDL kinetic modeling in rats, which is preferable in pharmacological or longitudinal studies.

Original languageEnglish
Pages (from-to)730-738
Number of pages9
JournalMolecular Imaging and Biology
Volume15
Issue number6
Publication statusPublished - Dec-2013

    Keywords

  • [C-11]MDL 100907, PET, Serotonin, 5-HT2A receptor, Kinetic modeling, Reference tissue, REFERENCE TISSUE MODEL, HUMAN BRAIN, CORTEX, QUANTIFICATION, BEHAVIOR

ID: 5993995