Chemistry:SR-14968
From HandWiki
Short description: Chemical compound
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| Formula | C20H20BrCl2N3O |
| Molar mass | 469.20 g·mol−1 |
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SR-14968 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. It is closely related to other compounds such as brorphine and SR-17018. Similarly to brorphine, SR-14968 shows robust biased agonist activity in vitro, but in animal studies in vivo behaves more like a typical opioid agonist at higher dose ranges, though still with a superior safety profile compared to unbiased agonists such as fentanyl. Compounds of this class are under development as potential analgesic medications with lower risk of overdose and drug dependence compared to traditional opioid drugs.[1][2][3][4][5]
See also
References
- ↑ "Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics". Cell 171 (5): 1165–1175.e13. November 2017. doi:10.1016/j.cell.2017.10.035. PMID 29149605.
- ↑ "Effectiveness comparisons of G-protein biased and unbiased mu opioid receptor ligands in warm water tail-withdrawal and drug discrimination in male and female rats". Neuropharmacology 150: 200–209. May 2019. doi:10.1016/j.neuropharm.2019.01.020. PMID 30660628.
- ↑ "G protein signaling-biased mu opioid receptor agonists that produce sustained G protein activation are noncompetitive agonists". Proceedings of the National Academy of Sciences of the United States of America 118 (48). November 2021. doi:10.1073/pnas.2102178118. PMID 34819362. Bibcode: 2021PNAS..11802178S.
- ↑ "Comparison of an Addictive Potential of μ-Opioid Receptor Agonists with G Protein Bias: Behavioral and Molecular Modeling Studies". Pharmaceutics 14 (1): 55. December 2021. doi:10.3390/pharmaceutics14010055. PMID 35056950.
- ↑ "Biased Opioid Ligands: Revolution or Evolution?". Frontiers in Pain Research (Lausanne, Switzerland) 2: 722820. 2021. doi:10.3389/fpain.2021.722820. PMID 35295469.
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