Chemistry:BU09059
From HandWiki
Short description: Chemical compound
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| Formula | C28H37N3O5 |
| Molar mass | 495.620 g·mol−1 |
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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
- κ-Opioid receptor § Antagonists
- List of investigational antidepressants
References
- ↑ 1.0 1.1 1.2 "Characterization of BU09059: a novel potent selective κ-receptor antagonist". ACS Chemical Neuroscience 5 (3): 177–84. March 2014. doi:10.1021/cn4001507. PMID 24410326.
- ↑ 2.0 2.1 "Antagonists of the kappa opioid receptor". Bioorganic & Medicinal Chemistry Letters 24 (9): 2021–32. May 2014. doi:10.1016/j.bmcl.2014.03.040. PMID 24690494.
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