Literature DB >> 27889455

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

Jaya Prabhakaran1, Kiran Kumar Solingapuram Sai2, Francesca Zanderigo1, Harry Rubin-Falcone3, Matthew J Jorgensen4, Jay R Kaplan4, Katharine I Tooke3, Akiva Mintz2, J John Mann1, J S Dileep Kumar5.   

Abstract

We recently reported the radiosynthesis and in vitro evaluation of [18F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([18F]FECIMBI-36) or ([18F]1), an agonist radioligand for 5HT2A/2C receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [18F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [18F]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 [18F]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT2A/2C receptors by PET. Copyright Â
© 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  5-HT; 5-HT(2A/2C)R; Agonist; PET; Radiotracer

Mesh：

Substances：

Year:  2016        PMID： 27889455      PMCID： PMC5348621          DOI： 10.1016/j.bmcl.2016.11.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


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