Chemistry:14-Methoxymetopon
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| Formula | C19H23NO4 |
| Molar mass | 329.396 g·mol−1 |
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14-Methoxymetopon is an experimental opioid drug developed by a team led by Professor Helmut Schmidhammer at the University of Innsbruck in the mid-1990s.[1] It is a derivative of metopon in which a methoxy group has been inserted at the 14-position. It is a highly potent analgesic drug that is around 500 times stronger than morphine when administered systemically; however, when given spinally or supraspinally, it exhibits analgesic activity up to a million fold greater than morphine.[2] It binds strongly to the μ-opioid receptor and activates it to a greater extent than most similar opioid drugs.[3] This produces an unusual pharmacological profile, and although 14-methoxymetopon acts as a potent μ-opioid full agonist in regard to some effects such as analgesia, a ceiling effect is seen on other effects such as constipation and respiratory depression which is believed to involve interaction with the κ-opioid receptor[4]
See also
References
- ↑ "Agonist compounds" US patent 5886001
- ↑ "14-Methoxymetopon, a very potent mu-opioid receptor-selective analgesic with an unusual pharmacological profile". European Journal of Pharmacology 459 (2–3): 203–9. January 2003. doi:10.1016/S0014-2999(02)02821-2. PMID 12524147.
- ↑ "Separation of binding affinity and intrinsic activity of the potent mu-opioid 14-methoxymetopon". The Journal of Pharmacology and Experimental Therapeutics 319 (1): 247–53. October 2006. doi:10.1124/jpet.106.105395. PMID 16801454.
- ↑ "14-methoxymetopon, a potent opioid, induces no respiratory depression, less sedation, and less bradycardia than sufentanil in the dog". Anesthesia and Analgesia 90 (6): 1359–64. June 2000. doi:10.1097/00000539-200006000-00018. PMID 10825321.
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