{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,22]],"date-time":"2026-10-22T02:52:37Z","timestamp":1792637557974,"version":"4.5.0"},"reference-count":40,"publisher":"SAGE Publications","issue":"1","license":[{"start":{"date-parts":[[2011,8,31]],"date-time":"2011-08-31T00:00:00Z","timestamp":1314748800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":["journals.sagepub.com"],"crossmark-restriction":true},"short-container-title":["J Cereb Blood Flow Metab"],"published-print":{"date-parts":[[2012,1]]},"abstract":"\n [\n 11<\/jats:sup>\n C]PHNO is a D\n 2<\/jats:sub>\n \/D\n 3<\/jats:sub>\n agonist positron emission tomography radiotracer, with higher in vivo affinity for D\n 3<\/jats:sub>\n than for D\n 2<\/jats:sub>\n receptors. As [\n 11<\/jats:sup>\n C]-( + )-PHNO is an agonist, its in vivo binding is expected to be more affected by acute fluctuations in synaptic dopamine than that of antagonist radiotracers such as [\n 11<\/jats:sup>\n C]raclopride. In this study, the authors compared the effects of an oral dose of the dopamine releaser amphetamine (0.3 mg\/kg) on in vivo binding of [\n 11<\/jats:sup>\n C]-( + )-PHNO and [\n 11<\/jats:sup>\n C]raclopride in healthy subjects, using a within-subjects, counterbalanced, open-label design. In the dorsal striatum, where the density of D\n 3<\/jats:sub>\n receptors is negligible and both tracers predominantly bind to D2 receptors, the reduction of [\n 11<\/jats:sup>\n C]-( + )-PHNO binding potential ( BP\n ND<\/jats:sub>\n ) was 1.5 times larger than that of [\n 11<\/jats:sup>\n C]raclopride. The gain in sensitivity associated with the agonist [\n 11<\/jats:sup>\n C]-( + )-PHNO implies that ~65% of D\n 2<\/jats:sub>\n receptors are in the high-affinity state in vivo. In extrastriatal regions, where [\n 11<\/jats:sup>\n C]-( + )-PHNO predominantly binds to D\n 3<\/jats:sub>\n receptors, the amphetamine effect on [\n 11<\/jats:sup>\n C]-( + )-PHNO BP\n ND<\/jats:sub>\n was even larger, consistent with the higher affinity of dopamine for D\n 3<\/jats:sub>\n . This study indicates that [\n 11<\/jats:sup>\n C]- ( + )-PHNO is superior to [\n 11<\/jats:sup>\n C]raclopride for studying acute fluctuations in synaptic dopamine in the human striatum. [\n 11<\/jats:sup>\n C]-( + )-PHNO also enables measurement of synaptic dopamine in D\n 3<\/jats:sub>\n regions.\n <\/jats:p>","DOI":"10.1038\/jcbfm.2011.115","type":"journal-article","created":{"date-parts":[[2011,8,31]],"date-time":"2011-08-31T04:07:56Z","timestamp":1314763676000},"page":"127-136","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":128,"title":["Within-Subject Comparison of [\n 11<\/sup>\n C]-( + )-PHNO and [\n 11<\/sup>\n C]raclopride Sensitivity to Acute Amphetamine Challenge in Healthy Humans"],"prefix":"10.1177","volume":"32","author":[{"given":"Paul","family":"Shotbolt","sequence":"first","affiliation":[{"name":"GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK"},{"name":"Department of Neurosciences, Imperial College, Hammersmith Hospital Campus, London, UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andri 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