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Towards NR2B receptor selective imaging agents for PET—synthesis and evaluation ofN-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

Authors
Journal
Bioorganic & Medicinal Chemistry
0968-0896
Publisher
Elsevier
Publication Date
Volume
14
Issue
18
Identifiers
DOI: 10.1016/j.bmc.2006.05.046
Keywords
  • Pet
  • Nmda-Nr2B
  • Glutamate
  • Amidine
  • Carbon-11

Abstract

Abstract Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.

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