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The 14‐Alkyl‐ and 14‐Alkenyl‐5 β ‐methylindolomorphinan Series Provide δ ‐Selective Partial Opioid Agonists
Author(s) -
Grundt Peter,
MartinezBermejo Fernando,
Lewis John W.,
Husbands Stephen M.
Publication year - 2003
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.200390080
Subject(s) - chemistry , partial agonist , opioid , agonist , alkyl , stereochemistry , opioid receptor , receptor , pharmacology , biochemistry , organic chemistry , medicine
A series of 14 β ‐alkyl‐ and 14 β ‐alkenyl‐5 β ‐methylindolomorphinans was synthesized and evaluated in opioid binding and functional assays. While being relatively nonselective in binding assays, the 14‐cinnamyl and 14‐isopentyl members showed selective opioid δ ‐receptor partial agonist activity in [ 35 S]GTP γ S assays.
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