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

在非人灵长类动物中对 [(18)F]FECIMBI-36(一种 5-HT(2A/2C) 受体激动剂 PET 放射性配体)进行体内评估

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Abstract

We recently reported the radiosynthesis and in vitro evaluation of [(18)F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([(18)F]FECIMBI-36) or ([(18)F]1), an agonist radioligand for 5HT(2A/2C) receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [(18)F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [(18)F]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 [(18)F]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT(2A/2C) receptors by PET.

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