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

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-HT1A binding in vivo using both [11C]CUMI-101 (agonist)...

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Bibliographic Details
Published in:Journal of Pharmacological Sciences 2012, Vol.120(3), pp.254-257
Main Authors: Kumar, J.S. Dileep, Milak, Matthew S., Majo, Vattoly J., Prabhakaran, Jaya, Mali, Pratap, Savenkova, Lyudmila, Mann, J. John, Parsey, Ramin V.
Format: Article
Language:English
Subjects:
5-HT1A receptor (5-HT1AR)
Animals
Brain - metabolism
brain imaging
Brain Mapping
Carbon Radioisotopes
Humans
Kinetics
Ligands
Nerve Tissue Proteins - metabolism
Papio
Piperazines - metabolism
Positron-Emission Tomography
Pyridines - metabolism
Receptor, Serotonin, 5-HT1A - metabolism
Serotonin 5-HT1 Receptor Agonists - metabolism
Serotonin 5-HT1 Receptor Antagonists - metabolism
Triazines - metabolism
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Summary: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-HT1A 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-HT1A receptor (5-HT1AR)-rich regions of baboon brain. The binding (BPF) 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-HT1AR ligands previously reported.
ISSN:1347-8613
1347-8648
DOI:10.1254/jphs.12100SC