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RB-64

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
RB-64
Legal status
Legal status
  • Legal/Uncontrolled
Identifiers
  • 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
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC24H27NO8S
Molar mass489.54 g·mol−1
3D model (JSmol)
  • C[C@@]12CC[C@H]3C(=O)O[C@@H](C[C@@]3([C@H]1C(=O)[C@H](C[C@H]2C(=O)OC)OC(=O)CSC#N)C)C4=COC=C4
  • InChI=1S/C24H27NO8S/c1-23-6-4-14-22(29)33-17(13-5-7-31-10-13)9-24(14,2)20(23)19(27)16(8-15(23)21(28)30-3)32-18(26)11-34-12-25/h5,7,10,14-17,20H,4,6,8-9,11H2,1-3H3/t14-,15-,16-,17-,20-,23-,24-/m0/s1 checkY[PubChem]
  • Key:AZPUAKGNQXURGA-ZWLNRFIDSA-N checkY[PubChem]

RB-64 is a semi-syntheticderivative ofsalvinorin A. It is anirreversible agonist, with a reactivethiocyanate group that forms abond to theκ-opioid receptor (KOR), resulting in very high potency.[1] It isfunctionally selective, activatingG proteins more potently thanβ-arrestin-2.[2] RB-64 has abias factor of up to 96 and isanalgesic with fewer of the side-effects associated with unbiased KOR agonists.[3] The analgesia is long-lasting. Compared with unbiased agonists, RB-64 evokes considerably lessreceptor internalization.

See also

[edit]

References

[edit]
  1. ^Yan F, Bikbulatov RV, Mocanu V, Dicheva N, Parker CE, Wetsel WC, et al. (July 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):6898–6908.doi:10.1021/bi900605n.PMC 2752672.PMID 19555087.
  2. ^White KL, Scopton AP, Rives ML, Bikbulatov RV, Polepally PR, Brown PJ, 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.
  3. ^White KL, Robinson JE, Zhu H, DiBerto JF, Polepally PR, Zjawiony JK, et al. (January 2015)."The G protein-biased κ-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo".The Journal of Pharmacology and Experimental Therapeutics.352 (1):98–109.doi:10.1124/jpet.114.216820.PMC 4279099.PMID 25320048.
μ-opioid
(MOR)
Agonists
(abridged;
full list)
Antagonists
δ-opioid
(DOR)
Agonists
Antagonists
κ-opioid
(KOR)
Agonists
Antagonists
Nociceptin
(NOP)
Agonists
Antagonists
Others


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