Biological Activity
Opioid analgesia is accompanied by side effects including tolerance, respiratory depression, constipation, and opioid induced hyperalgesia (OIH), which primarily mediated via the activation of μ receptors. Research suggest that the detrimental effects might be minimised by restricting β-arrestin2 recruitment to the μ receptor. SR17018 is a high-efficacy activator of G-protein signalling with limited capacity to stimulate β-arrestin2 recruitment largely through a non-competitive agonist action
[1].
References
[1] Singleton, S., Dieterle, C., Walker, D. J., Runeberg, T., Oswald, A. S., Rosenqvist, G., Robertson, L., McCarthy, T., Sarkar, S., Baptista-Hon, D., & Hales, T. G. (2024). Activation of μ receptors by SR-17018 through a distinctive mechanism. Neuropharmacology, 258, Article 110093.
https://doi.org/10.1016/j.neuropharm.2024.110093
