AGONIST AND ANTAGONIST ACTIVITIES OF LIGANDS DERIVED FROM NALTREXONE AND OXYMORPHONE

被引：88

作者：

TAKEMORI, AE ^{[1
]}

SULTANA, M ^{[1
]}

NAGASE, H ^{[1
]}

PORTOGHESE, PS ^{[1
]}

机构：

[1] UNIV MINNESOTA,COLL PHARM,DEPT MED CHEM,MINNEAPOLIS,MN 55455

来源：

LIFE SCIENCES | 1992年 / 50卷 / 20期

关键词：

D O I：

10.1016/0024-3205(92)90138-F

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The pharmacological profile of naltrindole (NTI) and three of its analogues, N-methyl-NTI (N-Me-NTI), oxymorphindole (OMI) and naltriben (NTB) were studied in antinociceptive assays. The compounds were found to have agonist activities that appear to be mediated mainly by kappa-opioid receptors because nor-binaltorphimine (nor-BNI), the selective kappa-opioid receptor antagonist inhibited their effects significantly. All of the compounds, behaved as antagonists at doses that were lower than those that produced agonist effects and they possessed a profile that was very selective for inhibiting the antinociceptive activities of delta-opioid receptor agonists. Differential antagonism by NTB of the activities of DSLET and DPDPE was demonstrated.

引用

页码：1491 / 1495

页数：5

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