title: In vivo evaluation of [18F]FECIMBI-36, an agonist 5-HT2A/2Creceptor PET radioligand in nonhuman primate.
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/2Creceptors 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/2Creceptors by PET.
authors.affiliation: Department of Psychiatry, Columbia University Medical Center, New York, USA; Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA.
authors.forename: Jaya
authors.initials: J
authors.lastname: Prabhakaran
authors.affiliation: Department of Radiology, Wake Forest School of Medicine, Winston-Salem, NC, USA.
authors.forename: Kiran Kumar
authors.initials: KK
authors.lastname: Solingapuram Sai
authors.affiliation: Department of Psychiatry, Columbia University Medical Center, New York, USA; Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA.
authors.forename: Francesca
authors.initials: F
authors.lastname: Zanderigo
authors.affiliation: Department of Psychiatry, Columbia University Medical Center, New York, USA.
authors.forename: Harry
authors.initials: H
authors.lastname: Rubin-Falcone
authors.affiliation: Department of Pathology, Section on Comparative Medicine, Wake Forest School of Medicine, Winston-Salem, NC, USA.
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Jorgensen
authors.affiliation: Department of Pathology, Section on Comparative Medicine, Wake Forest School of Medicine, Winston-Salem, NC, USA.
authors.forename: Jay R
authors.initials: JR
authors.lastname: Kaplan
authors.affiliation: Department of Psychiatry, Columbia University Medical Center, New York, USA.
authors.forename: Katharine I
authors.initials: KI
authors.lastname: Tooke
authors.affiliation: Department of Radiology, Wake Forest School of Medicine, Winston-Salem, NC, USA.
authors.forename: Akiva
authors.initials: A
authors.lastname: Mintz
authors.affiliation: Department of Psychiatry, Columbia University Medical Center, New York, USA; Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA.
authors.forename: J John
authors.initials: JJ
authors.lastname: Mann
authors.affiliation: Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA. Electronic address: kumardi@nyspi.columbia.edu.
authors.forename: J S Dileep
authors.initials: JSD
authors.lastname: Kumar
mesh_terms: D000818:Animals; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D008279:Magnetic Resonance Imaging; D008297:Male; D015394:Molecular Structure; D049268:Positron-Emission Tomography; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism*; D058826:Serotonin 5-HT2 Receptor Agonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C000607832:((18)F)-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine; D005021:Ethylamines; D005462:Fluorine Radioisotopes; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D058826:Serotonin 5-HT2 Receptor Agonists
keywords: 5-HT; 5-HT(2A/2C)R; Agonist; PET; Radiotracer