PMID: 7855175Jan 1, 1993Paper

PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor

Psychopharmacology
P KarlssonB Skrumsager

Abstract

The benzazepines NNC 687 and NNC 756 have in animal studies been described as selective D1-dopamine receptor antagonists. Both compounds have been labeled with 11C for examination by positron emission tomography (PET). In the present study central receptor binding was studied in monkeys and healthy men. After IV injection of both radioligands in Cynomolgus monkeys radioactivity accumulated markedly in the striatum, a region with a high density of D1-dopamine receptors. This striatal uptake was displaced by high doses of the selective D1-antagonist SCH 23390 (2 mg/kg) but not by the 5HT2-antagonist ketanserin (1.5 mg/kg) or the selective D2-antagonist raclopride (3 mg/kg). The cortical uptake after injection of [11C]NNC 687 was not reduced in displacement experiments with ketanserin. The cortical uptake of [11C]NNC 756 was reduced in displacement and protection experiments with ketanserin by 24-28% (1.5 mg/kg), whereas no reduction could be demonstrated on striatal uptake. In healthy males both compounds accumulated markedly in the striatum. For [11C]NNC 687 the ratio of radioactivity in the putamen to cerebellum was about 1.5. For [11C]NNC 756 the ratio was about 5. This ratio of 5 for [11C]NNC 756 is the highest obtained so fa...Continue Reading

References

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Citations

Oct 24, 2012·Psychopharmacology·Akihiro TakanoLars Farde
Mar 21, 2009·European Journal of Nuclear Medicine and Molecular Imaging·Akihiro TakanoChrister Halldin
May 14, 2009·European Journal of Nuclear Medicine and Molecular Imaging·Andrea VarroneLars Farde
Dec 3, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Magnus SchouChrister Halldin
May 25, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Julie A McCarronLars Farde
May 3, 2007·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Jesper EkelundMarc Laruelle
Mar 1, 1996·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·J N DaSilvaS Houle
May 10, 2005·Nuclear Medicine and Biology·Sjoerd J FinnemaChrister Halldin
Aug 28, 1998·Nuclear Medicine and Biology·C FogedL Farde
May 27, 2014·Nuclear Medicine and Biology·F GourandC Halldin
Jul 3, 2013·Nuclear Medicine and Biology·Anu J AiraksinenChrister Halldin
Dec 15, 2011·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Sjoerd J FinnemaLars Farde
Mar 4, 2000·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·A Abi-DarghamM Laruelle

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