In vivo evaluation of [F]FECIMBI-36, an agonist 5-HT receptor PET radioligand in nonhuman primate.

Bioorg Med Chem Lett 2017 01 16;27(1):21-23. Epub 2016 Nov 16.

Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA. Electronic address:

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

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http://dx.doi.org/10.1016/j.bmcl.2016.11.043DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5348621PMC
January 2017
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