Chemistry:R-30490
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| Formula | C24H32N2O2 |
| Molar mass | 380.532 g·mol−1 |
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R-30490 (also known as 4-methoxymethylfentanyl) is an opioid analgesic related to the highly potent animal tranquilizer carfentanil, and with only slightly lower potency. It was first synthesised by a team of chemists at Janssen Pharmaceutica led by Paul Janssen, who were investigating the structure-activity relationships of the fentanyl family of drugs. R-30490 was found to be the most selective agonist for the μ-opioid receptor out of all the fentanyl analogues tested, but it has never been introduced for medical use in humans, although the closely related drug sufentanil is widely used for analgesia and anesthesia during major surgery.[2][3][4][5]
Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.[6]
See also
References
- ↑ Drug Enforecement Administration, Department of Justice (February 2018). "Schedules of Controlled Substances:Temporary Placement of Fentanyl-Related Substances in Schedule I. Temporary amendment; temporary scheduling order". Federal Register 83 (25): 5188–92. PMID 29932611.
- ↑ "Molecular determinants of mu receptor recognition for the fentanyl class of compounds". Molecular Pharmacology 41 (1): 185–96. January 1992. PMID 1310142.
- ↑ "Pharmacological profiles of fentanyl analogs at mu, delta and kappa opiate receptors". European Journal of Pharmacology 213 (2): 219–25. March 1992. doi:10.1016/0014-2999(92)90685-W. PMID 1355735.
- ↑ "Pharmacotherapy of opioids: present and future developments". Pharmacy World & Science 18 (1): 1–15. January 1996. doi:10.1007/BF00449683. PMID 8861825.
- ↑ "Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor". Journal of Medicinal Chemistry 43 (3): 381–91. February 2000. doi:10.1021/jm9903702. PMID 10669565.
- ↑ "Fentanyls: Are we missing the signs? Highly potent and on the rise in Europe". The International Journal on Drug Policy 26 (7): 626–31. July 2015. doi:10.1016/j.drugpo.2015.04.003. PMID 25976511. http://www.ijdp.org/article/S0955-3959%2815%2900097-3/abstract.
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