PMID: 8298574Nov 1, 1993Paper

11C]NNC 687 and [11C]NNC 756, dopamine D-1 receptor ligands. Preparation, autoradiography and PET investigation in monkey

Nuclear Medicine and Biology
C HalldinG Sedvall

Abstract

NNC 687 and NNC 756 [(+)-5-(2,3-dihydrobenzofuran-7-yl)-7-hydroxy-3-methyl- 8-nitro-2,3,4,5-tetrahydro-1H-3-benzazepine and (+)-8-chloro-5-(2,3-dihydrobenzofuran-7-yl)-7-hydroxy-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine] are two new potent dopamine D-1 receptor antagonists. [11C]NNC 687 and [11C]NNC 756 were both prepared by N-methylation of the corresponding desmethyl compounds with [11C]methyl iodide. The reactions were performed in acetone with subsequent normal-phase semi-preparative HPLC and resulting in 50-60% radiochemical yield (from EOB and decay-corrected) with a total synthesis time of 30-35 min and a radiochemical purity higher than 99%. The specific radioactivity obtained at time of injection was about 1500 Ci/mmol (55 GBq/mumol). Autoradiographic examination of [11C]NNC 687 and [11C]NNC 756 binding in post-mortem human brain sections showed specific binding in the striatum, a region with high density of dopamine D-1 receptors. PET examination of the radioligands in a Cynomolgus monkey demonstrated accumulation of radioactivity predominantly in the striatum. The ratio between radioactivities in the striatum and the cerebellum was about 2 and 8 for [11C]NNC 687 and [11C]NNC 756 after 60 min. [11C]NNC 756 should ...Continue Reading

References

Jan 1, 1991·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·C HalldinG Sedvall
Jan 1, 1991·Journal of Neuroscience Methods·A PerssonG Sedvall
Dec 22, 1988·Nature·J R BunzowO Civelli
Jan 1, 1986·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·C HalldinG Sedvall

❮ Previous
Next ❯

Citations

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
Apr 4, 2002·Nuclear Medicine and Biology·Michael KassiouBernard Maziere
Aug 28, 1998·Nuclear Medicine and Biology·C FogedL Farde
Dec 24, 1998·Nuclear Medicine and Biology·H HallG Sedvall
Sep 28, 2010·Nuclear Medicine and Biology·Mikael PalnerAlan A Wilson
Feb 24, 2015·European Journal of Medicinal Chemistry·Ashish Radadiya, Anamik Shah
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
Jan 1, 1994·European Archives of Psychiatry and Clinical Neuroscience·G SedvallL Farde
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Olaf PranteAshutosh Banerjee

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.

Related Papers

International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes
C HalldinG Sedvall
International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes
C HalldinG Sedvall
© 2022 Meta ULC. All rights reserved