PMID: 3027000Jan 1, 1986Paper

Preparation of 11C-labelled SCH 23390 for the in vivo study of dopamine D-1 receptors using positron emission tomography

International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes
Christer HalldinG Sedvall

Abstract

The dopamine D-1 receptor antagonist, SCH 23390 ((R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3- benzazepin-7-ol), was labelled by alkylation of the desmethyl compound SCH 24518 ((R)-(+)-8-chloro-2,3,4,5-tetrahydro-5-phenyl-1H-3-benzazepin-7- ol) with [11C]methyl iodide. A multivariate optimization method, Simplex, was employed to obtain the optimal radiochemical yield. Both straight-phase and reversed-phase preparative HPLC were investigated in the purification of [11C]SCH 23390. Reaction in acetone with subsequent straight-phase LC separation resulted in 80% radiochemical yield, based on [11C]methyl iodide, with a total synthesis time of 35-40 min and a radiochemical purity greater than 99%. The average specific activity was on the order of 11.1 GBq/mmol. The 11C-labelled SCH 23390 was used to visualize the dopamine D-1 receptor-rich areas of a monkey brain by positron emission tomography. The data obtained showed a rapid distribution of radioactivity into the brain and a conspicuous accumulation of [11C]SCH 23390 in the striatum.

References

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Citations

Jan 1, 1994·European Archives of Psychiatry and Clinical Neuroscience·G SedvallL Farde
May 3, 2007·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Jesper EkelundMarc Laruelle
Sep 1, 1994·Pharmacology, Biochemistry, and Behavior·T SumiyoshiK Shiba
Mar 1, 1992·Neurochemistry International·H HallG Sedvall
Jan 1, 1987·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·O T DeJesusA M Friedman
Jan 1, 1989·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·J UlinB Långström
Jan 1, 1989·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·S RamL D Spicer
Jan 1, 1990·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·V W PikeD J Silvester
Jan 1, 1991·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·C HalldinG Sedvall
Sep 1, 1992·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·R GailG Stöcklin
Jun 1, 1992·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·H F BeerP A Schubiger
Mar 1, 1996·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·J N DaSilvaS Houle
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Mar 1, 1993·Pharmacology & Toxicology·H HallG Sedvall
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