BU09059

BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR).[1][2] It was derived from the irreversible (long-acting) KOR antagonist JDTic in search of an antagonist with a reversible profile of inactivation of the KOR that could be used with less concern to treat psychiatric disorders.[1][2] In addition to its reversibility, BU09059 is much more selective for the KOR 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]

BU09059
Identifiers
Chemical and physical data
FormulaC28H37N3O5
Molar mass495.620 g·mol−1
3D model (JSmol)

See also

References
  1. Casal-Dominguez, Joseph J.; Furkert, Daniel; Ostovar, Mehrnoosh; Teintang, Linnea; Clark, Mary J.; Traynor, John R.; Husbands, Stephen. M.; Bailey, Sarah J. (March 2014). "Characterization of BU09059: A Novel Potent Selective κ-Receptor Antagonist". ACS Chemical Neuroscience. 5 (3): 177–184. doi:10.1021/cn4001507. ISSN 1948-7193. PMC 3963132. PMID 24410326.
  2. Urbano, Mariangela; Guerrero, Miguel; Rosen, Hugh; Roberts, Edward (May 2014). "Antagonists of the kappa opioid receptor". Bioorganic & Medicinal Chemistry Letters. 24 (9): 2021–2032. doi:10.1016/j.bmcl.2014.03.040. ISSN 0960-894X. PMID 24690494.


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