SR-17018
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Formula | C19H18Cl3N3O |
Molar mass | 410.72 g·mol−1 |
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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
[edit]References
[edit]- ^ Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, et al. (November 2022). "Molecular recognition of morphine and fentanyl by the human μ-opioid receptor". Cell. 185 (23): 4361–4375.e19. doi:10.1016/j.cell.2022.09.041. PMID 36368306. S2CID 253426623.
- ^ Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, et al. (January 2020). "A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal". Neuropsychopharmacology. 45 (2): 416–425. doi:10.1038/s41386-019-0491-8. PMC 6901606. PMID 31443104.
- ^ Azevedo Neto J, Costanzini A, De Giorgio R, Lambert DG, Ruzza C, Calò G (August 2020). "Biased versus Partial Agonism in the Search for Safer Opioid Analgesics". Molecules. 25 (17): 3870. doi:10.3390/molecules25173870. PMC 7504468. PMID 32854452.
- ^ Podlewska S, Bugno R, Kudla L, Bojarski AJ, Przewlocki R (October 2020). "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): 4636. doi:10.3390/molecules25204636. PMC 7594085. PMID 33053718.
- ^ Pantouli F, Grim TW, Schmid CL, Acevedo-Canabal A, Kennedy NM, Cameron MD, et al. (December 2020). "Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain". Neuropharmacology. 185: 108439. doi:10.1016/j.neuropharm.2020.108439. PMC 7887086. PMID 33345829. S2CID 229306872.