title: Validation and quantification of [18F]altanserin binding in the rat brain using blood input and reference tissue modeling.
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.
authors.affiliation: Molecular Imaging Chemistry Laboratory, Department of Clinical Neurosciences, University of Cambridge, Cambridge, UK.
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Riss
authors.forename: Young T
authors.initials: YT
authors.lastname: Hong
authors.forename: David
authors.initials: D
authors.lastname: Williamson
authors.forename: Daniele
authors.initials: D
authors.lastname: Caprioli
authors.forename: Sergey
authors.initials: S
authors.lastname: Sitnikov
authors.forename: Valentina
authors.initials: V
authors.lastname: Ferrari
authors.forename: Steve J
authors.initials: SJ
authors.lastname: Sawiak
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Baron
authors.forename: Jeffrey W
authors.initials: JW
authors.lastname: Dalley
authors.forename: Tim D
authors.initials: TD
authors.lastname: Fryer
authors.forename: Franklin I
authors.initials: FI
authors.lastname: Aigbirhio
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002531:Cerebellum / Q000000981:diagnostic imaging / Q000378:metabolism; D002560:Cerebrovascular Circulation / Q000502:physiology; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes / Q000737:chemistry; D007650:Ketanserin / Q000031:analogs & derivatives* / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D008954:Models, Biological; D049268:Positron-Emission Tomography; D011485:Protein Binding; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D012015:Reference Standards
chemical_list: D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D044402:Receptor, Serotonin, 5-HT2A; C071983:altanserin; D007650:Ketanserin