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 |
| Molar mass | 495.609 |
| |
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]
See also
References
- 1 2 3 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. doi:10.1021/cn4001507. ISSN 1948-7193. PMID 24410326.
- 1 2 Urbano, Mariangela; Guerrero, Miguel; Rosen, Hugh; Roberts, Edward (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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