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In Vivo Delineation of 5-HT_1A Receptors in Human Brain with [¹⁸F]MPPF

PET Center, Groningen University Hospital, Groningen; Groningen University Institute for Drug Exploration, Groningen, The Netherlands

View larger version (25K): [in this window] [in a new window]   FIGURE 1. Time–activity curves for several brain regions after intravenous injection of 79 MBq [18F]MPPF in single subject.

View larger version (91K): [in this window] [in a new window]   FIGURE 2. Comparison between distribution of [18F]MPPF and flow tracer [15O]H2O. For clarity, images were processed using gaussian filter (CAPP; Siemens/CTI). A = level of basal ganglia; B = level of medial temporal cortex.

View larger version (20K): [in this window] [in a new window]   FIGURE 3. Rate of metabolism of [18F]MPPF ( and dashed line represent fit) in single volunteer. Solid line represents metabolite-corrected arterial input function. Time interval from 0 to 10 min is shown in inset.

View larger version (14K): [in this window] [in a new window]   FIGURE 4. Radiochromatograms of [18F]MPPF-derived radioactivity in human plasma at 1, 5, and 40 min after injection. PM = polar metabolite.

View larger version (20K): [in this window] [in a new window]   FIGURE 5. Example of linear graphic analysis using Logan-Patlak fits. Slopes of fits represent the distribution volumes. ROI(T) refers to radioactivity in region of interest at time t. CER = cerebellum; Cp(t) = plasma radioactivity corrected for metabolites (23); 0T Cp(t)dt = integral of plasma radioactivity over time from time zero to time t; LTC = lateral temporal cortex; 0T ROI(t)dt = integral of radioactivity in region of interest over time from time zero to time t.

View larger version (16K): [in this window] [in a new window]   FIGURE 6. Correlation of distribution of [18F]MPPF in vivo with that of [3H]8-OH-2-(di-n-propylamino)tetralin in postmortem human brain (12). 1 = frontal cortex; 2 = cingulate cortex; 3 = insular cortex; 4 = medial temporal cortex (including hippocampal area).

View larger version (15K): [in this window] [in a new window]   FIGURE 7. Correlation of binding potentials (BP) of [18F]MPPF with those of [carbonyl-11C]WAY 100635 reported in literature (18,19). 1 = cingulate cortex; 2 = insular cortex; 3 = medial temporal cortex; 4 = frontal cortex; 5 = lateral temporal cortex.