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Contribution of ß-arrestin signaling to physiological effects of the studied receptors

Determine the contribution of ß-arrestin signaling to the physiological effects mediated by the seven transmembrane receptors investigated (vasopressin V2 receptor, C-X-C chemokine receptor 4, apelin receptor, mu opioid receptor, and glucagon-like peptide 1 receptor), to establish links between ß-arrestin inhibition and specific behavioral or physiological responses.

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Background

To provide an in vivo proof-of-concept, the authors used morphine analgesia where the role of ß-arrestin 2 is known, showing ARIP potentiates morphine’s effect in rats.

They note that, for many of the other receptors studied, the role of ß-arrestin signaling in driving particular physiological responses has not yet been defined, which constrains broader translational interpretation.

References

However, to do so, the link between ß-arrestin inhibition and a particular physiological response must first have been established; for many of the 7TMRs in our panel, the contribution of ß-arrestin signalling to their various physiological effects has yet to be determined.

— A lipidated peptide derived from the C-terminal tail of the vasopressin 2 receptor shows promise as a new $β$-arrestin inhibitor (2411.07258 - Brouillette et al., 2 Nov 2024) in Section 3.6