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Validation and Quantification of [18F]Altanserin Binding in the Rat Brain Using Blood Input and Reference Tissue Modeling
Author(s) -
Patrick J. Riss,
Young T. Hong,
David J. Williamson,
Daniele Caprioli,
Sergey Sitnikov,
Valentina Ferrari,
Stephen J. Sawiak,
JeanClaude Baron,
Jeffrey W. Dalley,
Tim D. Fryer,
Franklin I. Aigbirhio
Publication year - 2011
Publication title -
journal of cerebral blood flow and metabolism
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.167
H-Index - 193
eISSN - 1559-7016
pISSN - 0271-678X
DOI - 10.1038/jcbfm.2011.94
Subject(s) - positron emission tomography , metabolite , brain tissue , cerebellum , chemistry , tissue distribution , distribution (mathematics) , medicine , endocrinology , nuclear medicine , biology , biochemistry , mathematics , mathematical analysis
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.

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