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

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

来源：Journal of Pharmacological Sciences, 2012, 120(3): 254-257.

DOI：10.1254/jphs.12100SC

• 5-HT1A receptor (5-HT1AR)
• positron emission tomography
• brain imaging

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 [C-11]CUM1-101 (agonist) and [C-11]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 [C-11]CUMI-101 was lower on an average of 55% across the regions of interest (ROIs) compared to [C-11]WAY100635. This ratio is consistent with the in vitro binding data of agonist and antagonist 5-HT1AR ligands previously reported.

• 出版日期2012-11