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Quantification of D2-Like Dopamine Receptors in the Human Brain with 18F-Desmethoxyfallypride

Gerhard Gründer, MD1, Thomas Siessmeier, MD2, Markus Piel, PhD3, Ingo Vernaleken, MD1, Hans-Georg Buchholz, BSc2, Yun Zhou, PhD4, Christoph Hiemke, PhD1, Dean F. Wong, MD, PhD4, Frank Rösch, PhD3 and Peter Bartenstein, MD2

1 Department of Psychiatry, University of Mainz, Mainz, Germany
2 Department of Nuclear Medicine, University of Mainz, Mainz, Germany
3 Institute of Nuclear Chemistry, University of Mainz, Mainz, Germany
4 Division of Nuclear Medicine, Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, Maryland



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FIGURE 1. Fraction of unchanged 18F-DMFP over scanning time of 124 min (n = 10; mean ± SD).

 


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FIGURE 2. Typical thin-layer chromatograms for 18F-DMFP and metabolite(s) 10 min (top) and 60 min (bottom) after injection, respectively. 1 = Metabolite; 2 = intact 18F-DMFP.

 


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FIGURE 3. Typical set of time–activity curves in putamen ({blacktriangleup}), thalamus ({blacksquare}), and cerebellum (•) with fitted curves (solid lines) obtained in healthy human volunteer. Dashed lines represent specific binding in putamen (long dashes) and in thalamus (short dashes), when specific binding in these structures is expressed as difference between total binding in structure and cerebellum. From 3-compartment, 5-parameter model, rate constants in putamen in this subject were determined as follows: K1 = 0.405 mL/min/mL; k2 = 0.077/min; k3 = 0.862/min; k4 = 0.338/min.

 


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FIGURE 4. Time–activity curves in putamen ({blacktriangleup}) and cerebellum (•) with fitted curves (solid lines) obtained in schizophrenic patient, who was treated with benzamide antipsychotic amisulpride (1,000 mg/d), which is also highly selective for D2 and D3 DA receptors. Dashed line represents specific binding in putamen, when specific binding in this structure is expressed as difference between total binding in structure and cerebellum. In this patient, scan duration was just 90 min.

 


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FIGURE 5. Correlations between VDs as determined with 3-compartment model and 2-compartment model (A) as well as between VDs as determined with 3-compartment model and Logan plot with arterial blood sampling (Logan invasive method; B).

 


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FIGURE 6. Correlations between BPs as determined with 3-compartment model and reference tissue model (A) as well as between BPs as determined with transient equilibrium model and reference tissue model (B).

 





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