Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity

• Published in: EJNMMI research Vol. 9; no. 1; pp. 1 - 8
• Main Authors: Lindberg, Anton, Arakawa, Ryosuke, Nogami, Tsuyoshi, Nag, Sangram, Schou, Magnus, Elmore, Charles S., Farde, Lars, Pike, Victor W., Halldin, Christer
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 21.11.2019; Springer Nature B.V; SpringerOpen
• Subjects: 5-HT1B; Affinity; Agonist; Agonists; Antagonist; Binding; Brain; Cardiac Imaging; Change detection; Imaging; Ligands; Medicine; Medicine & Public Health; Nuclear Medicine; Oncology; Original Research; Orthopedics; PET; Positron emission; Radioligand; Radiology; Receptors; Sensitivity analysis; Tomography; Agonist; Radioligand; Antagonist; 5-HT; PET

Background Over the last decade, a few radioligands have been developed for PET imaging of brain 5-HT 1B receptors. The 5-HT 1B receptor is a G-protein-coupled receptor (GPCR) that exists in two different agonist affinity states. An agonist ligand is expected to be more sensitive towards competition...