Ethyl-5-methylnaloxone (7) and 14-0-ethyl-5-methylnaltrexone (8) have been prepared starting from 14-0-ethyl-5-methyloxycodone (9) in several steps. Both, 7 and 8, were found to be opioid antagonists in vitro and in vivo. Compound 7 exhibited some selectivity forp opioid receptors, whereas compound
Synthesis and Biological Evaluation of 14-Alkoxymorphinans. Part 10. 14-O-Methyl derivatives of 5-methylnaltrexone and 5-methylnaloxone
โ Scribed by Helmut Schmidhammer; Christine Nussbaumer; Dinesh Patel; John R. Traynor
- Publisher
- John Wiley and Sons
- Year
- 1994
- Tongue
- German
- Weight
- 265 KB
- Volume
- 77
- Category
- Article
- ISSN
- 0018-019X
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๐ SIMILAR VOLUMES
Introduction. -5-Methyloxymorphone ( = 14-hydroxymetopon; 1) was found to possess slightly less opioid-agonist properties than oxymorphone (2) [2]. When compared to the highly potent opioid agonist 14-0-methyloxymorphone (3
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## Abstract The 14โ__O__โbenzylnaltrexones **3**โ**6** were prepared from naltrexone (**2**) in several steps. The novel compounds were biologically evaluated in radioligand binding and in [^35^S]GTP__ฮณ__S functional assays in comparison to the reference compound naltrexone. In the binding assay, c
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