| Autor: |
Ghazanfari N; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., van Waarde A; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Doorduin J; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Sijbesma JWA; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Kominia M; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Koelewijn M; Symeres, Groningen 9747 AT, The Netherlands., Attia K; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Willemsen ATM; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Visser TJ; Symeres, Groningen 9747 AT, The Netherlands., Heeres A; Symeres, Groningen 9747 AT, The Netherlands., Dierckx RAJO; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., de Vries EFJ; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands., Elsinga PH; University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, University of Groningen, Groningen 9700 RB, The Netherlands. |
| Abstrakt: |
The histamine H 3 receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H 3 receptor antagonist [ 11 C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H 3 receptor density in animal models of neurodegenerative disease. [ 11 C]GSK-189254 was intravenously administered to healthy Wistar rats ( n = 10), and a 60 min dynamic PET scan was carried out. Arterial blood samples were obtained during the scan to generate a metabolite-corrected plasma input function. PET data were analyzed using a one-tissue compartment model (1T2k), irreversible (2T3k) or reversible two-tissue compartment models (2T4k), graphical analysis (Logan and Patlak), reference tissue models (SRTM and SRTM2), and standard uptake values (SUVs). The Akaike information criterion and the standard error of the estimated parameters were used to select the most optimal quantification method. This study demonstrated that the 2T4k model with a fixed blood volume fraction and Logan graphical analysis can best describe the kinetics of [ 11 C]GSK-189254 in the rat brain. SUV 40-60 and the reference tissue-based measurements DVR(2T4k), BP ND (SRTM), and SUV ratio could also be used as a simplified method to estimate H 3 receptor availability in case blood sampling is not feasible. |
