Chemistry:Quadazocine
From HandWiki
Short description: Chemical compound
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| Formula | C25H37NO2 |
| Molar mass | 383.576 g·mol−1 |
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Quadazocine (WIN-44,441) is an opioid antagonist of the benzomorphan family which is used in scientific research.[1] It acts as a silent antagonist at all three of the major opioid receptors—μ, κ, and δ,[1][2] but with a significant preference in affinity for the μ receptor and the κ2 subtype.[3][4][5] As such, it has been touted as a "κ2-selective" antagonist, though this is not entirely accurate on account of its similar affinity for the μ receptor.[3][5] As would be expected, quadazocine reverses the effects (e.g., analgesia) of opioid agonists like morphine and fentanyl in animals.[1][6]
See also
References
- ↑ 1.0 1.1 1.2 "Multiple opioid receptor profile in vitro and activity in vivo of the potent opioid antagonist Win 44,441-3". Life Sciences 33 (Suppl 1): 303–6. 1983. doi:10.1016/0024-3205(83)90503-9. PMID 6319882.
- ↑ "Pharmacological profiles of opioid ligands at kappa opioid receptors". BMC Pharmacology 6: 3. 2006. doi:10.1186/1471-2210-6-3. PMID 16433932.
- ↑ 3.0 3.1 "Pharmacological characterization of opioid delta and kappa receptors". Pharmacology of Opioid Peptides. CRC Press. 1 September 1995. p. 238. ISBN 978-3-7186-5632-5. https://books.google.com/books?id=PhHTwIy9Wd8C&pg=PA238. Retrieved 22 April 2012.
- ↑ Drug Addiction: From Basic Research to Therapy. Springer. 13 June 2008. p. 421. ISBN 978-0-387-76677-5. https://books.google.com/books?id=Z36GjK1vABEC&pg=PA421. Retrieved 22 April 2012.
- ↑ 5.0 5.1 "Effects of U50488 and bremazocine on [Ca2+]i and cAMP in naive and tolerant rat ventricular myocytes: evidence of kappa opioid receptor multiplicity in the heart". Journal of Molecular and Cellular Cardiology 31 (2): 355–62. February 1999. doi:10.1006/jmcc.1998.9998. PMID 10093048.
- ↑ "Sex differences in opioid antinociception in rhesus monkeys: antagonism of fentanyl and U50,488 by quadazocine". The Journal of Pain 3 (3): 218–26. June 2002. doi:10.1054/jpai.2002.124734. PMID 14622776.
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