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
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Identifiers | |
ATC code | none |
PubChem | CID 73347341 |
ChemSpider | 30812525 ![]() |
ChEMBL | CHEMBL2381583 ![]() |
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[edit]
References[edit]
- ^ White K, Robinson JE, Zhu H, et al. (January 2015). "The G Protein–Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic with a Unique Spectrum of Activities In Vivo". Journal of Pharmacology and Experimental Therapeutics. 352 (1): 98–109. doi:10.1124/jpet.114.216820. PMC 4279099
. PMID 25320048.
Further reading[edit]
- Yan F, Bikbulatov RV, Mocanu V, et al. (July 2009). "Structure-Based Design, Synthesis, and Biochemical and Pharmacological Characterization of Novel Salvinorin A Analogues as Active State Probes of the κ-Opioid Receptor". Biochemistry. 48 (29): 6898–908. doi:10.1021/bi900605n. PMC 2752672
. PMID 19555087.
- White KL, Scopton AP, Rives ML, et al. (January 2014). "Identification of Novel Functionally Selective κ-Opioid Receptor Scaffolds". Molecular Pharmacology. 85 (1): 83–90. doi:10.1124/mol.113.089649. PMC 3868907
. PMID 24113749.
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