Validation and quantification of [18F]altanserin binding in the rat brain using blood input and reference tissue modeling

被引:19
作者
Riss, Patrick J. [1 ,2 ,3 ]
Hong, Young T. [1 ,4 ]
Williamson, David [1 ,4 ]
Caprioli, Daniele [3 ,5 ]
Sitnikov, Sergey [4 ,6 ]
Ferrari, Valentina [1 ,2 ]
Sawiak, Steve J. [1 ,3 ,4 ]
Baron, Jean-Claude [3 ,6 ,7 ]
Dalley, Jeffrey W. [3 ,5 ,8 ]
Fryer, Tim D. [1 ,3 ,4 ]
Aigbirhio, Franklin I. [1 ,2 ,3 ,4 ]
机构
[1] Univ Cambridge, Wolfson Brain Imaging Ctr, Dept Clin Neurosci, Cambridge CB2 0QQ, England
[2] Univ Cambridge, Mol Imaging Chem Lab, Dept Clin Neurosci, Cambridge CB2 0QQ, England
[3] Univ Cambridge, Behav & Clin Neurosci Inst, Cambridge CB2 0QQ, England
[4] Univ Cambridge, Lab Mol Imaging, Dept Clin Neurosci, Cambridge CB2 0QQ, England
[5] Univ Cambridge, Dept Expt Psychol, Cambridge CB2 0QQ, England
[6] Univ Cambridge, Dept Clin Neurosci, Neurol Unit, Cambridge CB2 0QQ, England
[7] Univ Paris, INSERM, U894, Ctr Psychiat & Neurosci, F-75252 Paris, France
[8] Univ Cambridge, Dept Psychiat, Cambridge CB2 0QQ, England
基金
英国医学研究理事会;
关键词
F-18]altanserin; animal; brain; 5-HT2A; modeling; PET; POSITRON-EMISSION-TOMOGRAPHY; RECEPTOR-LIKE IMMUNOREACTIVITY; 5HT(2) RECEPTORS; BOLUS/INFUSION APPROACH; SEROTONIN RECEPTORS; 5-HT2A RECEPTORS; F-18; ALTANSERIN; PET DATA; DISORDER; LIGAND;
D O I
10.1038/jcbfm.2011.94
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
The 5-hydroxytryptamine type 2a (5-HT2A) selective radiotracer [F-18]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. [F-18]altanserin showed sufficient brain uptake in a distribution pattern consistent with the known distribution of 5-HT2A 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. [F-18]altanserin is suitable for quantification of 5-HT2A receptor availability in rats. Journal of Cerebral Blood Flow & Metabolism (2011) 31, 2334-2342; doi:10.1038/jcbfm.2011.94; published online 13 July 2011
引用
收藏
页码:2334 / 2342
页数:9
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