Quadazocine
 | |
| Clinical data | |
|---|---|
| ATC code | None |
| Identifiers | |
| |
| CAS Number | 69924-29-4 |
| PubChem (CID) | 115077 |
| ChemSpider | 102983 |
| UNII |
X9BMD58553  |
| Chemical and physical data | |
| Formula | C25H37NO2 |
| Molar mass | 383.567 g/mol |
| 3D model (Jmol) | Interactive image |
| |
| |
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, of course, 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 2 3 Ward SJ, Pierson AK, Michne WF (1983). "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. doi:10.1016/0024-3205(83)90503-9. PMID 6319882.
- ↑ Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J (2006). "Pharmacological profiles of opioid ligands at kappa opioid receptors". BMC Pharmacology. 6: 3. doi:10.1186/1471-2210-6-3. PMC 1403760
. PMID 16433932. - 1 2 Leon F. Tseng (1 September 1995). Pharmacology of Opioid Peptides. CRC Press. p. 238. ISBN 978-3-7186-5632-5. Retrieved 22 April 2012.
- ↑ Rao S. Rapaka; Wolfgang Sadée (13 June 2008). Drug Addiction: From Basic Research to Therapy. Springer. p. 421. ISBN 978-0-387-76677-5. Retrieved 22 April 2012.
- 1 2 Zhang WM, Wu S, Yu XC, Wang HX, Bian JS, Wong TM (February 1999). "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. doi:10.1006/jmcc.1998.9998. PMID 10093048.
- ↑ Negus SS, Zuzga DS, Mello NK (June 2002). "Sex differences in opioid antinociception in rhesus monkeys: antagonism of fentanyl and U50,488 by quadazocine". The Journal of Pain : Official Journal of the American Pain Society. 3 (3): 218–26. doi:10.1054/jpai.2002.124734. PMID 14622776.
This article is issued from Wikipedia - version of the 10/25/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.