title: Autoradiographic Evaluation of [(18)F]FECUMI-101, a High Affinity 5-HT1AR Ligand in Human Brain.
abstract: [(18)F]FECUMI-101 ([(18)F]1) is a 5HT1AR ligand demonstrating specific binding in brain regions corresponding to the distribution of 5-HT1AR in baboons. However, we detected moderate uptake of [(18)F]1 in baboon thalamus, a brain region lacking 5-HT1AR. We sought to investigate the relative binding of [(18)F]1 to 5-HT1AR, α1R, and 5-HT7R in vitro. Using autoradiography in human brain sections, specific binding of [(18)F]1 to 5-HT1AR was confirmed. However, [(18)F]1 also showed 26% binding to α1R in PFC. The hippocampal formation exhibited 51% and 92% binding of [(18)F]1 to α1R and 5-HT1AR, respectively. Thalamus and cerebellum showed very little binding. There is no measurable specific binding of [(18)F]1 to 5-HT7R and no effect of temperature on [(18)F]1 specific binding to 5-HT1AR or α1R. These results indicate that, while [(18)F]FECUMI-101 is not a completely selective 5-HT1AR ligand for receptor quantification, it may be useful for occupancy measurements of drugs acting at 5-HT1AR in vivo.
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, New York 10032, United States; Department of Psychiatry, Stony Brook University School of Medicine, Stony Brook, New York 11794, United States.
authors.forename: J S Dileep
authors.initials: JS
authors.lastname: Kumar
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, New York 10032, United States; Department of Psychiatry, Columbia University Medical Center, New York, New York 10032, United States.
authors.forename: Mark D
authors.initials: MD
authors.lastname: Underwood
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute , New York, New York 10032, United States.
authors.forename: Norman R
authors.initials: NR
authors.lastname: Simpson
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute , New York, New York 10032, United States.
authors.forename: Suham A
authors.initials: SA
authors.lastname: Kassir
authors.affiliation: Department of Psychiatry, Columbia University Medical Center , New York, New York 10032, United States.
authors.forename: Jaya
authors.initials: J
authors.lastname: Prabhakaran
authors.affiliation: Department of Psychiatry, Columbia University Medical Center , New York, New York 10032, United States.
authors.forename: Vattoly J
authors.initials: VJ
authors.lastname: Majo
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute , New York, New York 10032, United States.
authors.forename: Mihran J
authors.initials: MJ
authors.lastname: Bakalian
authors.affiliation: Department of Psychiatry, Stony Brook University School of Medicine , Stony Brook, New York 11794, United States.
authors.forename: Ramin V
authors.initials: RV
authors.lastname: Parsey
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, New York 10032, United States; Department of Psychiatry, Columbia University Medical Center, New York, New York 10032, United States.
authors.forename: J John
authors.initials: JJ
authors.lastname: Mann
authors.affiliation: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, New York 10032, United States; Department of Psychiatry, Columbia University Medical Center, New York, New York 10032, United States.
authors.forename: Victoria
authors.initials: V
authors.lastname: Arango
keywords: 5-HT1AR; PET; autoradiography; hippocampus; radiotracer; α1R