6-bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids

被引:51
作者
Marder, M
Viola, H
Wasowski, C
Wolfman, C
Waterman, PG
Cassels, BK
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,STRATHCLYDE INST DRUG RES,GLASGOW G1 1XW,LANARK,SCOTLAND
[4] UNIV STRATHCLYDE,DEPT PHARMACEUT SCI,GLASGOW G1 1XW,LANARK,SCOTLAND
[5] UNIV CHILE,FAC CIENCIAS,DEPT QUIM,SANTIAGO 1,CHILE
关键词
D O I
10.1006/bbrc.1996.0903
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
6-Bromoflavone, obtained by bromination of flavanone, binds to central benzodiazepine receptors with a Ki = 70 nM and has a clear anxiolytic activity in mice, at 0.5 mg/kg, i.p. A survey of the structure/affinity relationship for those receptors in a series of natural and synthetic flavonoids is presented. (C) 1996 Academic Press, Inc.
引用
收藏
页码:384 / 389
页数:6
相关论文
共 14 条
[1]   H-1 AND C-13 ASSIGNMENTS FROM SENSITIVITY-ENHANCED DETECTION OF HETERONUCLEAR MULTIPLE-BOND CONNECTIVITY BY 2D MULTIPLE QUANTUM NMR [J].
BAX, A ;
SUMMERS, MF .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1986, 108 (08) :2093-2094
[2]   INTERACTION OF CONVULSIVE LIGANDS WITH BENZODIAZEPINE RECEPTORS [J].
BRAESTRUP, C ;
SCHMIECHEN, R ;
NEEF, G ;
NIELSEN, M ;
PETERSEN, EN .
SCIENCE, 1982, 216 (4551) :1241-1243
[3]   INVIVO AND INVITRO MODULATION OF CENTRAL TYPE BENZODIAZEPINE RECEPTORS BY PHOSPHATIDYLSERINE [J].
DESTEIN, ML ;
MEDINA, JH ;
DEROBERTIS, E .
MOLECULAR BRAIN RESEARCH, 1989, 5 (01) :9-15
[4]  
HABERLEIN H, 1994, PHARMAZIE, V49, P912
[5]   6,3'-DINITROFLAVONE, A NOVEL HIGH-AFFINITY LIGAND FOR THE BENZODIAZEPINE RECEPTOR WITH POTENT ANXIOLYTIC PROPERTIES [J].
MARDER, M ;
VIOLA, H ;
WASOWSKI, C ;
WOLFMAN, C ;
WATERMAN, PG ;
MEDINA, JH ;
PALADINI, AC .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (22) :2717-2720
[6]  
MARDER M, IN PRESS PHYTOMEDICI
[7]   CHRYSIN (5,7-DI-OH-FLAVONE), A NATURALLY-OCCURRING LIGAND FOR BENZODIAZEPINE RECEPTORS, WITH ANTICONVULSANT PROPERTIES [J].
MEDINA, JH ;
PALADINI, AC ;
WOLFMAN, C ;
DESTEIN, ML ;
CALVO, D ;
DIAZ, LE ;
PENA, C .
BIOCHEMICAL PHARMACOLOGY, 1990, 40 (10) :2227-2231
[8]  
MEDINA JH, 1985, J NEUROCHEM, V44, P1340
[9]  
QUADER MA, 1991, TETRAHEDRON, V47, P3611
[10]  
SHEN XL, 1994, ACTA PHARMACOLOGICA, V15, P5