6,3'-DINITROFLAVONE, A NOVEL HIGH-AFFINITY LIGAND FOR THE BENZODIAZEPINE RECEPTOR WITH POTENT ANXIOLYTIC PROPERTIES

被引：39

作者：

MARDER, M

VIOLA, H

WASOWSKI, C

WOLFMAN, C

WATERMAN, PG

MEDINA, JH

PALADINI, AC

机构：

[1] UNIV BUENOS AIRES,FAC FARM & BIOQUIM,INST QUIM & FISICOQUIM BIOL,RA-1113 BUENOS AIRES,DF,ARGENTINA

[2] UNIV BUENOS AIRES,FAC MED,INST BIOL CELULAR,RA-1121 BUENOS AIRES,DF,ARGENTINA

[3] UNIV STRATHCLYDE,DEPT PHARMACEUT SCI,GLASGOW G1 1XW,LANARK,SCOTLAND

[4] STRATHCLYDE INST DRUG RES,PHYTOCHEM RES LABS,GLASGOW G1 1XW,LANARK,SCOTLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00464-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

6,3'-Dinitroflavone (2) and 6,4'-dinitroflavone (3), prepared by direct nitration of flavone (1), were found to be ligands for the benzodiazepine receptor (BDZ-R). Compound 2, with a K-i= 12 nM, produced potent anxiolytic effects in mice at a dose of 1 mu g/Kg.

引用

页码：2717 / 2720

页数：4

共 10 条

[1] SYNTHESIS AND BIOCHEMICAL EVALUATION OF A SERIES OF AMINOFLAVONES AS POTENTIAL INHIBITORS OF PROTEIN-TYROSINE KINASES P56(LCK), EGFR, AND P60(V-SRC) [J].