Quadazocine Explained

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,^[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. As would be expected, quadazocine reverses the effects (e.g., analgesia) of opioid agonists like morphine and fentanyl in animals.^[6]

See also

• Dezocine

Notes and References

1. Ward SJ, Pierson AK, Michne WF . Multiple opioid receptor profile in vitro and activity in vivo of the potent opioid antagonist Win 44,441-3 . Life Sciences . 33 . 303–6 . 1983 . Suppl 1 . 6319882 . 10.1016/0024-3205(83)90503-9.
2. Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J . Pharmacological profiles of opioid ligands at kappa opioid receptors . BMC Pharmacology . 6 . 3 . 2006 . 16433932 . 1403760 . 10.1186/1471-2210-6-3 . free .
3. Book: Porreca F . Pharmacological characterization of opioid delta and kappa receptors . Tseng LF . Pharmacology of Opioid Peptides . https://books.google.com/books?id=PhHTwIy9Wd8C&pg=PA238 . 22 April 2012 . 1 September 1995 . CRC Press . 978-3-7186-5632-5 . 238.
4. Book: Rapaka RS, Sadée W . Drug Addiction: From Basic Research to Therapy . 22 April 2012 . 13 June 2008 . Springer . 978-0-387-76677-5 . 421.
5. Zhang WM, Wu S, Yu XC, Wang HX, Bian JS, Wong TM . 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 . 10093048 . 10.1006/jmcc.1998.9998 .
6. Negus SS, Zuzga DS, Mello NK . 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 . 14622776 . 10.1054/jpai.2002.124734. free .