title: Autoradiographic evaluation of [3H]CUMI-101, a novel, selective 5-HT1AR ligand in human and baboon brain.
abstract: [11C]CUMI-101 is the first selective serotonin receptor (5-HT1AR) partial agonist radiotracer for positron emission tomography (PET) tested in vivo in nonhuman primates and humans. We evaluated specific binding of [3H]CUMI-101 by quantitative autoradiography studies in postmortem baboon and human brain sections using the 5-HT1AR antagonist WAY-100635 as a displacer. The regional and laminar distributions of [3H]CUMI-101 binding in baboon and human brain sections matched the known distribution of [3H]8-OH-DPAT and [3H]WAY-100635. Prazosin did not measurably displace [3H]CUMI-101 binding in baboon or human brain sections, thereby ruling out [3H]CUMI-101 binding to α1-adrenergic receptors. This study demonstrates that [11C]CUMI-101 is a selective 5-HT1AR ligand for in vivo and in vitro studies in baboon and human brain.
authors: Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA. kumardi@nyspi.columbia.edu
authors: J S Dileep
authors: JS
authors: Kumar
authors: Ramin V
authors: RV
authors: Parsey
authors: Suham A
authors: SA
authors: Kassir
authors: Vattoly J
authors: VJ
authors: Majo
authors: Matthew S
authors: MS
authors: Milak
authors: Jaya
authors: J
authors: Prabhakaran
authors: Norman R
authors: NR
authors: Simpson
authors: Mark D
authors: MD
authors: Underwood
authors: J John
authors: JJ
authors: Mann
authors: Victoria
authors: V
authors: Arango
mesh_terms: D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000033:anatomy & histology / Q000000981:diagnostic imaging / Q000378:metabolism*; D054333:Drug Partial Agonism; D006801:Humans; D008024:Ligands; D010215:Papio; D010879:Piperazines / Q000378:metabolism*; D049268:Positron-Emission Tomography; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D058825:Serotonin 5-HT1 Receptor Agonists / Q000378:metabolism*; D014227:Triazines / Q000378:metabolism*; D014316:Tritium
chemical_list: C510616:(O-methyl-11C) 2-(4-(4-(3-methoxyphenyl)piperazin-1-yl)-butyl)-4-methyl-2H-(1,2,4)-triazine-3,5-dione; D008024:Ligands; D010879:Piperazines; D058825:Serotonin 5-HT1 Receptor Agonists; D014227:Triazines; D014316:Tritium; D044282:Receptor, Serotonin, 5-HT1A