Radiosynthesis and evaluation of [11 C] EMPA as a potential PET tracer for orexin 2 receptors

C Wang, CK Moseley, SM Carlin, CM Wilson…

Index: Wang, Changning; Moseley, Christian K.; Carlin, Stephen M.; Wilson, Colin M.; Neelamegam, Ramesh; Hooker, Jacob M. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3389 - 3392

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Citation Number: 7

Abstract

EMPA is a selective antagonist of orexin 2 (OX2) receptors. Previous literature with [3H]- EMPA suggest that it may be used as an imaging agent for OX2 receptors; however, brain penetration is known to be modest. To evaluate the potential of EMPA as a PET radiotracer in non-human primate (as a step to imaging in man), we radiolabeled EMPA with carbon-11. Radiosynthesis of [11C] N-ethyl-2-(N-(6-methoxypyridin-3-yl)-2-methylphenylsulfonamido) ...