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. Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, Cameron MD, Bannister TD, Bohn LM. Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics. Cell. 2017 Nov 16;171(5):1165-1175.e13. doi: 10.1016/j.cell.2017.10.035. PMID: 29149605; PMCID: PMC5731250.
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. Grim TW, Acevedo-Canabal A, Bohn LM. Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics. Biol Psychiatry. 2020 Jan 1;87(1):15-21. doi: 10.1016/j.biopsych.2019.10.020. Epub 2019 Oct 31. PMID: 31806082; PMCID: PMC6919561.}
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 .