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In vivo evaluation of [18F]FECIMBI-36, an agonist 5-HT2A/2C receptor PET radioligand in nonhuman primate
Authors:Jaya Prabhakaran  Kiran Kumar Solingapuram Sai  Francesca Zanderigo  Harry Rubin-Falcone  Matthew J. Jorgensen  Jay R. Kaplan  Katharine I. Tooke  Akiva Mintz  J. John Mann  J.S. Dileep Kumar
Affiliation:1. Department of Psychiatry, Columbia University Medical Center, New York, USA;2. Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA;3. Department of Radiology, Wake Forest School of Medicine, Winston-Salem, NC, USA;4. Department of Pathology, Section on Comparative Medicine, Wake Forest School of Medicine, Winston-Salem, NC, USA
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.
Keywords:5-HT  Agonist  PET  Radiotracer
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