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

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
Main Authors: J.S. Dileep Kumar, Matthew S. Milak, Vattoly J. Majo, Jaya Prabhakaran, Pratap Mali, Lyudmila Savenkova, J. John Mann, Ramin V. Parsey
Format: Article
Language:English
Published: Elsevier 2012-01-01
Series:Journal of Pharmacological Sciences
Online Access:http://www.sciencedirect.com/science/article/pii/S1347861319304402
Description
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. Keywords:: 5-HT1A receptor (5-HT1AR), positron emission tomography, brain imaging
ISSN:1347-8613

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