6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
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.
Marder
M
M
Instituto de Química y Fisicoquímica Biológicas, Facultad de Farmaciay Bioquímica, Buenos Aires, Argentina.
Viola
H
H
Wasowski
C
C
Wolfman
C
C
Waterman
P G
PG
Cassels
B K
BK
Medina
J G
JG
Paladini
A C
AC
D000345:Affinity Labels / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D000704:Analysis of Variance; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D005419:Flavonoids / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D005445:Flunitrazepam / Q000378:metabolism; D007700:Kinetics; D018782:Maze Learning / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
C099934:6-bromoflavone; D000345:Affinity Labels; D014151:Anti-Anxiety Agents; D005419:Flavonoids; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid; D005445:Flunitrazepam