Quantitative PET Analysis of the Dopamine D2 Receptor Agonist Radioligand

Quantitative PET Analysis of the Dopamine D2 Receptor Agonist Radioligand,Tatsui Otsuka,Hiroshi Ito,Christer Halldin,Hidehiko Takahashi,Harumasa Takan

Quantitative PET Analysis of the Dopamine D2 Receptor Agonist Radioligand  
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Tatsui Otsuka, Hiroshi Ito, Christer Halldin, Hidehiko Takahashi, Harumasa Takano, Ryosuke Arakawa, Masaki Okumura, Fumitoshi Kodaka, Michie Miyoshi, Mizuho Sekine, Chie Seki, Ryuji Nakao
in the human brain and analyzed using quantitative approaches with or without an arterial input function. Methods: A 90-min dy- namic PET scan was obtained for 10 healthy men after an intra- venous injection of 11C-MNPA. The binding potential (BPND) was calculated using the indirect kinetic method, a kinetic compart- ment analysis with a metabolite-corrected arterial input function. BPND was also calculated by the simplified reference tissue model (SRTM) and transient equilibrium methods, both with the cerebellumasthereferencebrainregion.Theresultsofthequan- titative methods were compared in a cross-validation approach. Results: The highest regional radioactivity was observed in the putamen. BPND values obtained by kinetic analysis were 0.82 6 0.09, 0.59 6 0.11, and 0.28 6 0.06, respectively, in the puta- men, caudate, and thalamus. BPND values obtained by the SRTM and transient equilibrium methods were in good agree- ment with those obtained by the indirect kinetic method (r 5 0.98 and r 5 0.93, respectively). For all quantification methods, the BPND values based on data acquired from 0 to 60 min were in good agreement with those based on data acquired from 0 to 90 min (r 5 0.90-0.99). Conclusion: The regional distribution of 11C-MNPA binding was in good agreement with previous PET studies of dopamine D2 receptors in the human brain using an- tagonist radioligands. The results support routine use of the SRTM and transient equilibrium methods, that is, methods that do not require an arterial input function and need a scan time of only about 60 min. 11C-MNPA should thus be useful for clinical research on the pathophysiology of neuropsychiatric disorders and estimation of dopamine D2 receptor occupancy by dopa- minergic drugs.
Published in 2009.
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