Quantitative In Vivo Imaging Of Adenosine A2A Receptors In The Human Brain Using 11C-SCH442416 PET: A Pilot Study - Info and Reading Options

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<h4 style="border:0px;margin:10px 0px;padding:0px;vertical-align:baseline;clear:both;line-height:28px;">Abstract</h4><h4 style="border:0px;margin:10px 0px;padding:0px;vertical-align:baseline;clear:both;line-height:28px;"></h4><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"></p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 was reported in preclinical studies with rodents and primates to be the first nonxanthine radioligand suitable for the <span>in vivo</span> imaging of adenosine A<span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">2A</span> receptors with positron emission tomography (PET). The aim of the present work was to investigate the suitability of <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 for the <span>in vivo</span> quantification of A<span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">2A</span> receptors in human brain.</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><b><span>Methods:</span> </b>Five male healthy subjects were scanned with 364 MBq bolus injections of <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416. 90 minutes of dynamic PET emission data were acquired, and arterial blood samples were taken throughout the scan to generate an arterial plasma input function. Using the individual MR images, regions-of-interest (ROIs) were defined for cerebellum, caudate, putamen and thalamus. Spectral analysis was used to determine the frequency components of the <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 tissue response for regional and voxel time-activity curves (TACs).</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><b><span>Results:</span> </b><span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 was rapidly metabolised in blood, the fraction of unmetabolised parent tracer in plasma being 41% at 15 minutes and 15% at 95 minutes, lower than that reported in rats and <span>macaca nemestrina</span>. No lipophilic radiolabelled metabolites were found in human plasma.</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;">Rapid uptake of <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 was observed in all brain regions, reaching a maximum at about 3 minutes. When spectral analysis was applied to regional brain time activity curves (TACs), relatively rapid reversible region dependent and slower irreversible, region independent but subject specific components were identified. These components were further separated into irreversible nonspecific binding, reversible nonspecific binding, reversible specific binding and a blood component. Binding potentials of the nondisplaceable binding <span>BPND</span> were calculated using cerebellar volume of distribution as an estimate of the reversible nondisplaceable binding across the entire brain. Mean binding potentials <span>BPND</span> were: 2.5 (putamen), 1.6 (caudate) and 0.5 (thalamus).</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><span><b>Conclusion:</b></span> Our study demonstrates that A<span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">2A</span> receptor binding can be quantified in striatal regions of the human brain with <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 PET. Despite the complex tracer kinetics and its low specific binding, reliable binding potentials could be estimated with spectral analysis.</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><span><b>Citation</b></span></p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;">Grachev ID, Doder M, Brooks DJ, Hinz R. Quantitative<span> in vivo</span> Imaging of Adenosine A<span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">2A</span> Receptors in the Human Brain Using <span style="border:0px;margin:0px;padding:0px;vertical-align:baseline;height:0px;line-height:0;">11</span>C-SCH442416 PET: A Pilot Study. <span>Journal of Diagnostic Imaging in Therapy</span>. 2014; 1(1): 1-19.</p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><span><a href="http://dx.doi.org/10.17229/jdit.2014-0620-001" rel="nofollow">http://dx.doi.org/10.17229/jdit.2014-0620-001</a></span></p><p style="border:0px;margin:1em 0px;padding:0px;vertical-align:baseline;"><br /></p>

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