In vivo evaluation of [18F]FECIMBI-36, an agonist 5-HT2A/2C receptor PET radioligand in nonhuman primate

We recently reported the radiosynthesis and in vitro evaluation of [F-18]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([F-18]FECIMBI-36) or ([F-18]1), an agonist radioligand for 5HT(2A/2C) receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [F-18]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [F-18]FECIMBI-36 penetrates the blood-brain barrier and a low retention of radioactivity is observed in monkey brain. Although the time activity curves indicate a somehow heterogeneous distribution of the radioligand in the brain, the low level of [F-18]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT2A/2C receptors by PET. (C) 2016 Elsevier Ltd. All rights reserved.