Role of saturability of noncovalent interactions in the analysis of the three-dimensional structure-opioid activity relationship

被引：0
|
作者：
Kuz'mina, N. E. [1 ]
Stan'kov, I. N. [1 ]
机构：
[1] State Res Inst Organ Chem & Technol, Moscow 111024, Russia
来源：
RUSSIAN CHEMICAL BULLETIN | 2012年 / 61卷 / 06期
关键词：
opioid activity; agonistic interactions; three-dimensional model for an opiate pharmacophore; pharmacophore element; pharmacophore region; saturability of noncovalent interactions; SALVINORIN-A ANALOGS; OPIATE PHARMACOPHORE; GENERAL-MODEL; RECEPTOR; REGIONS; PM3; CONFIGURATION; AGONIST; BINDING; ABILITY;
D O I：
10.1007/s11172-012-0164-9
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The effect of the saturability of noncovalent interactions on the character of opioid activity of opioid receptor ligands belonging to different structural classes was investigated. A three-dimensional model for an opiate pharmacophore was used to show that the involvement of pharmacophore elements, which are responsible for the agonist ligand binding to opioid receptors, in intramolecular interactions gives rise to antagonistic properties.
引用
收藏
页码：1207 / 1214
页数：8
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