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Autoradiographic evaluation of [3H]CUMI-101, a novel, selective 5-HT1AR ligand in human and baboon brain

2013; Elsevier BV; Volume: 1507; Linguagem: Inglês

10.1016/j.brainres.2013.02.035

1872-6240

J.S. Dileep Kumar, Ramin V. Parsey, Suham Kassir, Vattoly J. Majo, Matthew S. Milak, Jaya Prabhakaran, Norman R. Simpson, Mark D. Underwood, J. John Mann, Victoria Arango,

Neurotransmitter Receptor Influence on Behavior

[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.