SR-17018 explained

SR-17018 is a drug which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment.^[1] In animal studies it produces analgesic effects but with less respiratory depression and development of tolerance than conventional opioids.^{[2] [3] [4] [5]}

See also

• Bezitramide
• Brorphine
• J-113,397
• Oliceridine
• PZM21
• SR-14968
• SR-16435
• SHR9352
• TRV734

Notes and References

1. Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE . 6 . Molecular recognition of morphine and fentanyl by the human μ-opioid receptor . Cell . 185 . 23 . 4361–4375.e19 . November 2022 . 36368306 . 10.1016/j.cell.2022.09.041 . 253426623 . free .
2. Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM . 6 . A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal . Neuropsychopharmacology . 45 . 2 . 416–425 . January 2020 . 31443104 . 10.1038/s41386-019-0491-8 . 6901606 .
3. Azevedo Neto J, Costanzini A, De Giorgio R, Lambert DG, Ruzza C, Calò G . Biased versus Partial Agonism in the Search for Safer Opioid Analgesics . Molecules . 25 . 17 . August 2020 . 3870 . 32854452 . 10.3390/molecules25173870 . 7504468 . free .
4. Podlewska S, Bugno R, Kudla L, Bojarski AJ, Przewlocki R . Molecular Modeling of µ Opioid Receptor Ligands with Various Functional Properties: PZM21, SR-17018, Morphine, and Fentanyl-Simulated Interaction Patterns Confronted with Experimental Data . Molecules . 25 . 20 . October 2020 . 4636 . 33053718 . 10.3390/molecules25204636 . 7594085 . free .
5. Pantouli F, Grim TW, Schmid CL, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM . 6 . Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain . Neuropharmacology . 108439 . December 2020 . 185 . 33345829 . 10.1016/j.neuropharm.2020.108439 . 7887086 . 229306872 .