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BU72
Opioid analgesic drug From Wikipedia, the free encyclopedia
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BU72 is an extremely potent opioid used in pharmacological research.
 | This article may be too technical for most readers to understand. (March 2021) |
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Pharmacology
BU72 is an agonist for the μ-opioid receptor with exceptionally high binding affinity and potency, comparable to carfentanil.[1] It also has extremely high efficacy, giving a stronger maximal effect than the standard full agonist DAMGO.[2] In animal studies, it was found to be a potent analgesic (giving pain relief at very low doses), with a slow onset and long duration of action.[3][4]
BU72 was used to produce the first crystal structure of the active μ-opioid receptor,[1] and is now widely used to model the activation process.[5][6][7] In the crystal structure, BU72 appears to bond to the receptor covalently,[8][9] but this seems to be an experimental artifact, since the compound binds reversibly, and preventing bond formation has no effect on affinity.[1]
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Chemistry
BU72 is synthesized in several steps from thebaine.[10] Its stereochemistry has recently been revised, with the phenyl group in the (R) configuration.[11][12]
See also
References
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