BU09059

BU09059

BU09059
Systematic (IUPAC) name
[1-ethoxy-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-1-oxopropan-2-yl] (3R)-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
Chemical data
Formula C28H37N3O5
Molecular mass 495.609

BU09059 is a potent and selective, reversible (short-acting) antagonist of the κ-opioid receptor (KOR).[1][2] It was derived from the irreversible KOR antagonist JDTic in search of an antagonist with a reversible profile of inactivation of the KOR that could be used to treat psychiatric disorders.[1][2] In addition to its reversibility, BU09059 is much more selective than JDTic, showing 15-fold and 616-fold preference for the KOR over the μ- and δ-opioid receptors (Ki = 1.72 nM, 26.5 nM, and 1060 nM, respectively).[1]

See also

References

  1. ^ a b c Casal-Dominguez, Joseph J.; Furkert, Daniel; Ostovar, Mehrnoosh; Teintang, Linnea; Clark, Mary J.; Traynor, John R.; Husbands, Stephen. M.; Bailey, Sarah J. (2014). "Characterization of BU09059: A Novel Potent Selective κ-Receptor Antagonist". ACS Chemical Neuroscience 5 (3): 177–184.  
  2. ^ a b Urbano, Mariangela; Guerrero, Miguel; Rosen, Hugh; Roberts, Edward (2014). "Antagonists of the kappa opioid receptor". Bioorganic & Medicinal Chemistry Letters 24 (9): 2021–2032.