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pubmed-article:8584610pubmed:abstractTextSCH 39166 is the first selective D1-dopamine receptor antagonist developed for clinical trials in schizophrenia. SCH 39166 was evaluated as a radioligand for PET, labeled with 11C, and as a D1-dopamine receptor antagonist after single oral doses in healthy men. After intravenous injection of [11C]SCH 39166 distribution of radioactivity in brain grossly reflected D1-dopamine receptor density. The putamen to cerebellum ratio at equilibrium was low (1.54 +/- 0.18 SD), which makes [11C]SCH 39166 less suitable as a radioligand for applied PET studies. Saturability of specific binding was demonstrated after IV injection of [11C]SCH 39166 with low specific radioactivity. Stereospecificity of binding was examined using the stereoisomer [11C]SCH 39165. D1-Receptor occupancy was demonstrated with [11C]SCH 39166 2 h after administration of single oral doses of unlabeled SCH 39166 to each of three healthy subjects (25, 100 and 400 mg). There was a substantial reduction of specific [11C]SCH 39166 uptake in the putamen after all doses. Single oral doses of 100 mg induced approximately 70% D1-dopamine receptor occupancy in the basal ganglia, which should be sufficient to investigate the antipsychotic potential of D1-dopamine receptor antagonism in clinical studies.lld:pubmed
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pubmed-article:8584610pubmed:pagination300-8lld:pubmed
pubmed-article:8584610pubmed:dateRevised2007-11-14lld:pubmed
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pubmed-article:8584610pubmed:articleTitleEvaluation of SCH 39166 as PET ligand for central D1 dopamine receptor binding and occupancy in man.lld:pubmed
pubmed-article:8584610pubmed:affiliationDepartment of Clinical Neuroscience, Karolinska Institutet, Stockholm, Sweden.lld:pubmed
pubmed-article:8584610pubmed:publicationTypeJournal Articlelld:pubmed
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pubmed-article:8584610pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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