Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes.

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➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology

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