Radiosynthesis and preclinical evaluation of 18F-F13714 as a fluorinated 5-HT1A receptor agonist radioligand for PET neuroimaging

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Laëtitia LemoineLuc Zimmer

Abstract

PET brain imaging of the serotonin 1A (5-hydroxytryptamine 1A [5-HT(1A)]) receptor has been widely used in clinical studies. Currently, only a few well-validated radiolabeled antagonist tracers are available for in vivo imaging of this central receptor. 5-HT(1A) receptors exist in high- and low-affinity states, depending on their coupling to G proteins. Agonists bind preferentially to receptors in the high-affinity state and thereby could provide a measure of functional 5-HT(1A) receptors. Therefore, it is of great interest to develop an (18)F-labeled full agonist 5-HT(1A) receptor radiotracer. In this study, we radiolabeled the high-affinity 5-HT(1A) receptor agonist (18)F-F13714 and investigated its potential as a PET tracer. F13714 nitro precursor was synthesized and radiolabeled via a fluoronucleophilic substitution. In vitro binding assays were performed using established protocols. Radiopharmacologic evaluations included in vitro autoradiography in rat brain and PET scans on anesthetized cats. The chemical and radiochemical purities of (18)F-F13714 were greater than 98%. F13714 has a high affinity (0.1 nM) and selectivity for 5-HT(1A) receptors. In vitro (18)F-F13714 binding in rats was consistent with the known 5-HT(1A) ...Continue Reading

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Citations

Jan 16, 2014·Neurobiology of Learning and Memory·Rudy Schreiber, Adrian Newman-Tancredi
Nov 5, 2019·Frontiers in Molecular Neuroscience·Matthieu ColomLuc Zimmer
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Luc Zimmer, Didier Le Bars
Mar 26, 2021·Frontiers in Neuroscience·Matthieu ColomLuc Zimmer
Aug 1, 2021·Drug Discovery Today·Krishna Kanta GhoshBalázs Gulyás
Dec 22, 2017·ACS Chemical Neuroscience·Magdalena Jastrzębska-WięsekAdrian Newman-Tancredi

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