Comparison of High and Low Affinity Serotonin 1A Receptors by PET In Vivo in Nonhuman Primates

J.S. Dileep Kumar; Matthew S. Milak; Vattoly J. Majo; Jaya Prabhakaran; Pratap Mali; Lyudmila Savenkova; J. John Mann; Ramin V. Parsey

doi:10.1254/jphs.12100SC

Short Communication

Comparison of High and Low Affinity Serotonin 1A Receptors by PET In Vivo in Nonhuman Primates

J.S. Dileep Kumar, Matthew S. Milak, Vattoly J. Majo, Jaya Prabhakaran, Pratap Mali, Lyudmila Savenkova, J. John Mann, Ramin V. Parsey

Author information

J.S. Dileep Kumar
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
New York State Psychiatric Institute, USA
Matthew S. Milak
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
New York State Psychiatric Institute, USA
Vattoly J. Majo
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
Jaya Prabhakaran
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
Pratap Mali
New York State Psychiatric Institute, USA
Lyudmila Savenkova
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
J. John Mann
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA
New York State Psychiatric Institute, USA
Department of Radiology, Columbia University College of Physicians and Surgeons, USA
Ramin V. Parsey
Department of Psychiatry and Behavioral Medicine, Stony Brook University, USA

Keywords: 5-HT_1A receptor (5-HT_1AR), positron emission tomography, brain imaging

JOURNAL FREE ACCESS

2012 Volume 120 Issue 3 Pages 254-257

DOI https://doi.org/10.1254/jphs.12100SC

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Abstract

Serotonin (5-HT) 1A receptors exist in high and low affinity states. Agonist ligands bind preferentially to the high affinity state receptors, providing a more functionally relevant measure than antagonist binding. We now report comparison of 5-HT_1A binding in vivo using both [¹¹C]CUMI-101 (agonist) and [¹¹C]WAY100635 (antagonist) in nonhuman primates. PET studies show that both tracers bind to known 5-HT_1A receptor (5-HT_1AR)-rich regions of baboon brain. The binding (BP_F) of [¹¹C]CUMI-101 was lower on an average of 55% across the regions of interest (ROIs) compared to [¹¹C]WAY100635. This ratio is consistent with the in vitro binding data of agonist and antagonist 5-HT_1AR ligands previously reported.

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