PMID: 8584610Oct 1, 1995Paper

Evaluation of SCH 39166 as PET ligand for central D1 dopamine receptor binding and occupancy in man

Psychopharmacology
P KarlssonL Farde

Abstract

SCH 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 antagoni...Continue Reading

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Citations

Oct 1, 1995·Psychopharmacology·T R Barnes, J Gerlach
Mar 4, 2006·European Journal of Nuclear Medicine and Molecular Imaging·Aurelija JucaiteLars Farde
Dec 3, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Magnus SchouChrister Halldin
Sep 19, 2008·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Magnus SchouChrister Halldin
Dec 22, 1999·Pharmacology & Therapeutics·G EmilienS Cragg
Aug 30, 2000·Nuclear Medicine and Biology·B AndréeL Farde
Aug 28, 1998·Nuclear Medicine and Biology·C FogedL Farde
Nov 13, 2002·The American Journal of Geriatric Psychiatry : Official Journal of the American Association for Geriatric Psychiatry·Saeeduddin AhmedWilliam Z Potter
May 9, 2006·Trends in Pharmacological Sciences·Chi-Ming Lee, Lars Farde

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