Synthesis and biological evaluation of 14-alkoxymorphinans .14. 14-ethoxy-9-methyl substituted indolomorphinans with delta opioid receptor selectivity

被引：14
作者：
Schmidhammer, H
Daurer, D
Wieser, M
Monory, K
Borsodi, A
Elliott, J
Traynor, JR
机构：
[1] BIOL RES CTR, INST BIOCHEM, H-6701 SZEGED, HUNGARY
[2] LOUGHBOROUGH UNIV TECHNOL, DEPT CHEM, LOUGHBOROUGH LE11 3TU, LEICS, ENGLAND
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 02期
关键词：
D O I：
10.1016/S0960-894X(96)00599-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The 5-methyl and 14-ethoxy substituted analogues (compounds 2-4) of the delta opioid receptor antagonist naltrindole showed similar selectivity when compared with the reference drug. Compound 2 was a delta 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 delta receptor agonist in the MVD. (C) 1997, Elsevier Science Ltd.
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页码：151 / 156
页数：6
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