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Synthesis and Biological Evaluation of 14‐Alkoxymorphinans Part 4 opioid agonists and partial opioid agonists in a series of N ‐(cyclobutylmethyl)‐14‐methoxymorphinan‐6‐ones
Author(s) -
Schmidhammer Helmut,
Burkard Willy P.,
EggsteinAeppli Lislott
Publication year - 1989
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19890720607
Subject(s) - chemistry , opioid , partial agonist , opioid receptor , pharmacology , stereochemistry , acetic acid , receptor , agonist , biochemistry , medicine
The N ‐(cyclobutylmethyl)morphinans 12 , 19 , 20 , 21 , 27 , and 29 and the N ‐(2‐cyanoethyl) analogue 33 were prepared from different precursors. Pharmacological evaluation ( e.g. opioid receptor binding assays, acetic‐acid writhing test, hot‐plate assay) points to a partial opioid agonism of compounds 12 , 27 , 29 , and 33 , and to full opioid agonism of compounds 19 – 21 .