Published in:
01-01-2020 | Image of the Month
18F-F13640 PET imaging of functional receptors in humans
Authors:
Matthieu Colom, Nicolas Costes, Jérôme Redouté, Frédéric Dailler, Florent Gobert, Didier Le Bars, Thierry Billard, Adrian Newman-Tancredi, Luc Zimmer
Published in:
European Journal of Nuclear Medicine and Molecular Imaging
|
Issue 1/2020
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Excerpt
The vast majority of PET radiopharmaceuticals used for receptor neuroimaging are antagonists. This is particularly true for 5-HT
1A receptor radiopharmaceuticals such as
18F-MPPF or
11C-WAY100635. These radiolabeled antagonists allow PET neuroimaging of the total pool of receptors, regardless of their functional state. In contrast, agonists bind preferentially to the functionally active state of receptors, a pharmacological property that has not yet been exploited for PET imaging of functional 5-HT
1A receptors [
1]. To this end, we have developed a highly selective 5-HT
1A receptor agonist,
18F-F13640, and validated it in animal models [
2]. A postmortem study in Alzheimer subjects showed that the in vitro binding of
18F-F13640 differs from that of
18F-MPPF, the prototypical radiopharmaceutical [
3]. …