14-Methoxymetopon
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14-Methoxymetopon
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| Systematic (IUPAC) name | |
| 3-hydroxy- 14-methoxy- 5,17-dimethyl- 7,8-dihydro- 4,5α- epoxy- morphinan- 6-one | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 131575-03-6  |
| ATC code | ? |
| PubChem | CID 5486940 |
| ChemSpider | 4589140  |
| ChEMBL | CHEMBL326684 |
| Synonyms | 14-Methoxymetopon |
| Chemical data | |
| Formula | C19H23NO4 |
| Mol. mass | 329.39 g/mol |
| SMILES | eMolecules & PubChem |
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14-Methoxymetopon is an opiate analogue that is a derivative of metopon which has been substituted with a methoxy group at the 14-position. It is a highly potent analgesic drug that is around 500x stronger than morphine when administered systemically; however, when given spinally or supraspinally, it exhibits analgesic activity up to a million fold greater than morphine.[1] It binds strongly to the μ-opioid receptor and activates it to a greater extent than most similar opioid drugs.[2] This produces an unusual pharmacological profile, and although 14-methoxymetopon acts as a potent μ-opioid full agonist in regards to some effects such as analgesia, a ceiling effect is seen on other effects such as constipation and respiratory depression.[3]
References
- ^ King, MA; Su, W; Nielan, CL; Chang, AH; Schütz, J; Schmidhammer, H; Pasternak, GW (2003). "14-Methoxymetopon, a very potent mu-opioid receptor-selective analgesic with an unusual pharmacological profile". European Journal of Pharmacology 459 (2–3): 203–9. doi:10.1016/S0014-2999(02)02821-2. PMID 12524147.
- ^ Mahurter, L; Garceau, C; Marino, J; Schmidhammer, H; Tóth, G; Pasternak, GW (2006). "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. doi:10.1124/jpet.106.105395. PMID 16801454.
- ^ Freye, E; Schmidhammer, H; Latasch, L (2000). "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. doi:10.1097/00000539-200006000-00018. PMID 10825321.
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