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RB-64

RB-64
22-thiocyanatosalvinorin A.svg
Clinical data
ATC code
  • none
Legal status
Legal status
  • Legal/Uncontrolled
Identifiers
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC24H27NO8S
Molar mass489.54 g/mol g·mol−1
3D model (JSmol)

RB-64 or 22-thiocyanatosalvinorin A is a semi-synthetic salvinorin 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

  1. ^ 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