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 | Zendy

Schmidhammer Helmut | Zendy; Burkard Willy P. | Zendy; EggsteinAeppli Lislott | Zendy

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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 .

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