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

Journal of Pharmacological Sciences

J. John Mann³  J.S. Dileep Kumar³  Ramin V. Parsey²  Jaya Prabhakaran³  Lyudmila Savenkova³  Vattoly J. Majo³  Pratap Mali¹  Matthew S. Milak³ 

[1] New York State Psychiatric Institute, USA;Department of Psychiatry and Behavioral Medicine, Stony Brook University, USA;Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University College of Physicians and Surgeons, USA

关键词: 5-HT1A receptor (5-HT1AR);    positron emission tomography;    brain imaging;   

DOI  :  10.1254/jphs.12100SC

学科分类：药学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(14)Cited-By(6)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.

【 授权许可】

Unknown