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Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with δ opioid receptor selectivity

✍ Scribed by Helmut Schmidhammer; Dietmar Daurer; Martina Wieser; Krisztina Monory; Anna Borsodi; Jackie Elliott; John R. Traynor

Book ID
104364742
Publisher
Elsevier Science
Year
1997
Tongue
English
Weight
264 KB
Volume
7
Category
Article
ISSN
0960-894X

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✦ Synopsis

The 5-methyl and 14-ethoxy substituted analogues (compounds 2 -4) of the 6 opioid receptor antagonist naltrindole showed similar selectivity when compared with the reference drug. Compound 2 was a 6 receptor antagonist in the mouse vas deferens preparation (MVD) exhibiting considerably higher selectivity ratios than naltrindole, while compound 4 was found to be a full and potent 8 receptor agonist in the MVD.

📜 SIMILAR VOLUMES

Synthesis and Biological Evaluation of 1
Synthesis and Biological Evaluation of 14-Alkoxymorphinans. Part 9. 14-O-ethyl-5-methylnaltrexone, and opioid antagonist with unusual selectivity
✍ Helmut Schmidhammer; Andrea Schratz; Charlotte Schmidt; Dinesh Patel; John R. Tr 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 German ⚖ 325 KB

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