Agonist and antagonist bind differently to 5-HT1A receptors during Alzheimer’s disease: A post-mortem study with PET radiopharmaceuticals

• Published in: Neuropharmacology Vol. 109; pp. 88 - 95
• Main Authors: Vidal, Benjamin, Sebti, Johan, Verdurand, Mathieu, Fieux, Sylvain, Billard, Thierry, Streichenberger, Nathalie, Troakes, Claire, Newman-Tancredi, Adrian, Zimmer, Luc
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.10.2016
• Subjects: 5-HT1A receptor; Aged; Aged, 80 and over; Alzheimer Disease - metabolism; Alzheimer Disease - pathology; Alzheimer’s disease; Autopsy; F13640; Female; Humans; Male; Middle Aged; MPPF; PET; Piperidines - metabolism; Positron-Emission Tomography; Protein Binding - physiology; Pyridines - metabolism; Radiopharmaceuticals - metabolism; Receptor, Serotonin, 5-HT1A - metabolism; Serotonin; Serotonin 5-HT1 Receptor Agonists - metabolism; Serotonin 5-HT1 Receptor Antagonists - metabolism; Alzheimer’s disease; Serotonin; MPPF; 5-HT1A receptor; PET; F13640; 5-HT(1A) receptor

PET imaging studies using 5-HT1A receptor radiotracers show a decreased density of this receptor in hippocampi of patients with Alzheimer’s disease (AD) at advanced stages. However, current 5-HT1A receptor radiopharmaceuticals used in neuroimaging are antagonists, thought to bind to 5-HT1A receptors...