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 7. 14,14′-dimethoxy analogues of norbinaltorphimine: Synthesis and determination of their χ opioid antagonist selectivity
✍ Scribed by Helmut Schmidhammer; Ernst Ganglbauer; Jörg Mitterdorfer; Judith M. Rollinger; Colin F. C. Smith
- Publisher
- John Wiley and Sons
- Year
- 1990
- Tongue
- German
- Weight
- 342 KB
- Volume
- 73
- Category
- Article
- ISSN
- 0018-019X
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✦ Synopsis
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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
## Abstract The 14‐__O__‐benzylnaltrexones **3**–**6** were prepared from naltrexone (**2**) in several steps. The novel compounds were biologically evaluated in radioligand binding and in [^35^S]GTP__γ__S functional assays in comparison to the reference compound naltrexone. In the binding assay, c