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Synthesis and Biological Evaluation of 14‐Alkoxymorphinans. Part 15. Novel δ opiod receptor antagonists with high affinity and selectivity in the 14‐alkoxy‐substituted indolomorphinan series
Author(s) -
Schmidhammer Helmut,
Krassnig Roland,
Greiner Elisabeth,
Schütz Johannes,
White Angela,
BerzeteiGurske Ilona P.
Publication year - 1998
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.19980810519
Subject(s) - chemistry , vas deferens , alkoxy group , potency , antagonist , selectivity , stereochemistry , receptor , indole test , opioid , pharmacology , combinatorial chemistry , in vitro , biochemistry , organic chemistry , alkyl , medicine , catalysis
The indolomorphinans 4 – 7 were prepared from their corresponding morphinan‐6‐one derivatives 8 – 11 via Fischer indole synthesis. Compounds 4 and 5 exhibited higher antagonist potency at δ opioid receptors in the mouse vas deferens preparation than the reference drug HS 378 ( 2 ), while compounds 6 and 7 were less potent.