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Pharmacology stubs
RB-64
Другие языки:

    RB-64

    Подписчиков: 0, рейтинг: 0
    RB-64
    22-thiocyanatosalvinorin A.svg
    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
    PubChem CID
    ChemSpider
    ChEMBL
    Chemical and physical data
    Formula C24H27NO8S
    Molar mass 489.54 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-synthetic derivative of salvinorin A. It is an irreversible agonist, with a reactive thiocyanate group that forms a bond to the κ-opioid receptor (KOR), resulting in very high potency. It is functionally selective, activating G proteins more potently than β-arrestin-2. RB-64 has a bias factor of up to 96 and is analgesic with fewer of the side-effects associated with unbiased KOR agonists. The analgesia is long-lasting. Compared with unbiased agonists, RB-64 evokes considerably less receptor internalization.

    See also


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