BU09059
BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR). 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. 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).
BU09059
BU09059 is a potent, selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor (KOR). 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. 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).
has abstract
BU09059 is a potent, selective ...... M, and 1060 nM, respectively).
@en
IUPAC name
ethyl 2-{[(3R)-7-hydroxy-1,2,3 ...... ethylpiperidin-1-yl]propanoate
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thumbnail
Wikipage page ID
46,402,118
Wikipage revision ID
731,075,554
smiles
CCOCCNC[C@H]3Cc4ccccc4CN3
StdInChIKey
RKGRJMYCISUSNK-XTNINKNLSA-N
hypernym
comment
BU09059 is a potent, selective ...... M, and 1060 nM, respectively).
@en
label
BU09059
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