Chemistry:SR-17018
From HandWiki
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] SR-17018 is also a noncompetitive opioid agonist.[6] It produces very little hyperactivity in mice, does not induce locomotor sensitization and counteracts the hyperactivity produced by morphine.[7]
See also
References
- ↑ "Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics". Cell 171 (5): 1165–75.e13. November 2017. doi:10.1016/j.cell.2017.10.035. PMID 29149605.
- ↑ "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. doi:10.1038/s41386-019-0491-8. PMID 31443104.
- ↑ "Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics". Biol Psychiatry 87 (1): 15–21. January 2020. doi:10.1016/j.biopsych.2019.10.020. PMID 31806082.
- ↑ "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. October 2020. doi:10.3390/molecules25204636. PMID 33053718.
- ↑ "Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain". Neuropharmacology 185. December 2020. doi:10.1016/j.neuropharm.2020.108439. PMID 33345829.
- ↑ "G protein signaling-biased mu opioid receptor agonists that produce sustained G protein activation are noncompetitive agonists". Proc Natl Acad Sci U S A 118 (48). November 2021. doi:10.1073/pnas.2102178118. PMID 34819362. Bibcode: 2021PNAS..11802178S.
- ↑ "Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine". Biomolecules 13 (6). June 2023. doi:10.3390/biom13060935. PMID 37371516.
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