Synthesis and biological evaluation of 14-alkoxymorphinans -: Part 15 -: Novel δ opioid receptor antagonists with high affinity and selectivity in the 14-alkoxy-substituted indolomorphinan series

被引:18
作者
Schmidhammer, H
Krassnig, R
Greiner, E
Schütz, J
White, A
Berzetei-Gurske, IP
机构
[1] Univ Innsbruck, Inst Pharmaceut Chem, A-6020 Innsbruck, Austria
[2] SRI Int, Div Pharmaceut, Menlo Pk, CA 94025 USA
关键词
D O I
10.1002/hlca.19980810519
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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 delta opioid receptors in the mouse vas deferens preparation than the reference drug HS 378 (2), while compounds 6 and 7 were less potent.
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页码:1064 / 1069
页数:6
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