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Serodolin, a β-arrestin–biased ligand of 5-HT 7 receptor, attenuates pain-related behaviors

Abstract : Transmembrane signaling through G protein–coupled receptors (GPCRs), originally described as requiring coupling to intracellular G proteins, also uses G protein–independent pathways through β-arrestin recruitment. Biased ligands, by favoring one of the multiple bioactive conformations of GPCRs, allow selective signaling through either of these pathways. Here, we identified Serodolin as the first β-arrestin–biased agonist of the serotonin 5-HT 7 receptor. This new ligand, while acting as an inverse agonist on G s signaling, selectively induces ERK activation in a β-arrestin–dependent way. Importantly, we report that Serodolin decreases pain intensity caused by thermal, mechanical, or inflammatory stimuli. Our findings suggest that targeting the 5-HT 7 R with β-arrestin–biased ligand could be a valid alternative strategy to the use of opioids for the relief of pain.
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https://hal.inrae.fr/hal-03684955
Contributor : Eric Reiter Connect in order to contact the contributor
Submitted on : Thursday, July 28, 2022 - 3:17:25 PM
Last modification on : Tuesday, September 27, 2022 - 4:10:38 AM

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Chayma El Khamlichi, Flora Reverchon, Nadège Hervouet-Coste, Elodie Robin, Nicolas Chopin, et al.. Serodolin, a β-arrestin–biased ligand of 5-HT 7 receptor, attenuates pain-related behaviors. Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2022, 119 (21), pp.1-12. ⟨10.1073/pnas.2118847119⟩. ⟨hal-03684955⟩

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