1. Validation and quantification of [18F]altanserin binding in the rat brain using blood input and reference tissue modeling.
- Author
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Riss PJ, Hong YT, Williamson D, Caprioli D, Sitnikov S, Ferrari V, Sawiak SJ, Baron JC, Dalley JW, Fryer TD, and Aigbirhio FI
- Subjects
- Animals, Brain diagnostic imaging, Cerebellum diagnostic imaging, Cerebellum metabolism, Cerebrovascular Circulation physiology, Chromatography, High Pressure Liquid, Fluorine Radioisotopes chemistry, Ketanserin blood, Ketanserin chemical synthesis, Ketanserin pharmacokinetics, Models, Biological, Positron-Emission Tomography, Protein Binding, Quality Control, Radiopharmaceuticals chemical synthesis, Rats, Receptor, Serotonin, 5-HT2A metabolism, Reference Standards, Brain metabolism, Ketanserin analogs & derivatives
- Abstract
The 5-hydroxytryptamine type 2a (5-HT(2A)) selective radiotracer [(18)F]altanserin has been subjected to a quantitative micro-positron emission tomography study in Lister Hooded rats. Metabolite-corrected plasma input modeling was compared with reference tissue modeling using the cerebellum as reference tissue. [(18)F]altanserin showed sufficient brain uptake in a distribution pattern consistent with the known distribution of 5-HT(2A) receptors. Full binding saturation and displacement was documented, and no significant uptake of radioactive metabolites was detected in the brain. Blood input as well as reference tissue models were equally appropriate to describe the radiotracer kinetics. [(18)F]altanserin is suitable for quantification of 5-HT(2A) receptor availability in rats.
- Published
- 2011
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