RB-64
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| Systematic (IUPAC) name | |
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Methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-9-(2-thiocyanatoacetyl)oxy-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylate | |
| Clinical data | |
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| Identifiers | |
| ATC code | None |
| PubChem | CID 73347341 |
| Chemical data | |
| Formula | C24H27NO8S |
| Molar mass | 489.54 g/mol |
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RB-64 or 22-thiocyanatosalvinorin A is a semi-synthetic salvonorin derivative and a κ-opioid receptor (KOR) agonist which is used in scientific research. Its most remarkable property is its biased activity in signal transduction in favour of G protein versus β-arrestin-2, a phenomenon which is called functional selectivity or biased agonism. RB-64 has a bias factor of 96 and is analgesic with fewer of the prototypical side-effects associated with unbiased KOR agonists. The analgesia-like effect is long-lasting. Compared with unbiased agonists RB-64 evokes considerably less receptor internalisation.[1]
See also
References
- ↑ White K, Robinson JE, Zhu H, et al. (2014). "The G-protein biased k-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo". J. Pharmacol. Exp. Ther. 352: 98–109. doi:10.1124/jpet.114.216820. PMID 25320048.
Further reading
- Yan F, Bikbulatov RV, Mocanu V, et al. (2009). "Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor". Biochemistry 48 (29): 6898–908. doi:10.1021/bi900605n. PMC 2752672. PMID 19555087.
- White KL, Scopton AP, Rives ML, et al. (2014). "Identification of novel functionally selective κ-opioid receptor scaffolds". Mol. Pharmacol. 85 (1): 83–90. doi:10.1124/mol.113.089649. PMID 24113749.
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