Behavioral effects of 6-bromoflavanone and 5-methoxy-6,8-dibromoflavanone as anxiolytic compounds.
Benzodiazepines (BDZs) are the most used psychoactive drugs in the pharmacotherapy of anxiety. A large number of structurally different classes of ligands are also active in the modulation of anxiety, showing high affinity for the benzodiazepine binding site (BDZ-bs) of the GABA (A) receptor complex. Various synthetic derivatives of natural flavonoids have been found to have very potent anxiolytic properties. This study was undertaken to provide a behavioral characterization of two novels halogenated flavonoids, 5-methoxy-6, 8-dibromoflavanone (FV1), and 6-bromoflavanone (FV2). These compounds were tested and compared to diazepam (0.5 mg/kg) and to the natural flavonoid chrysin (1 mg/kg) as a standard of activity. When injected in mice (0.5, 1 mg/kg i.p) both synthetic flavonoids increased the locomotor activity and the exploratory skills of the animals, as measured in the open-field and in the hole-board tests. Both compounds, indeed, had a clear anxiolytic activity in the elevated plus-maze, as measured by an increased number of entries and the percentage of time spent in the open arms. At the tested doses, both compounds did not induce sedative action or compulsive behaviour. These results encourage making deeper investigations on this field.
Ognibene
Elisa
E
Behavioural Neuroscience Section, Department of Cell Biology & Neuroscience, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161, Rome, Italy.
Bovicelli
Paolo
P
Adriani
Walter
W
Saso
Luciano
L
Laviola
Giovanni
G
D000704:Analysis of Variance; D000818:Animals; D014151:Anti-Anxiety Agents / Q000627:therapeutic use*; D001007:Anxiety / Q000188:drug therapy* / Q000503:physiopathology; D001522:Behavior, Animal / Q000187:drug effects*; D003975:Diazepam / Q000627:therapeutic use; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005106:Exploratory Behavior / Q000187:drug effects; D044950:Flavanones / Q000627:therapeutic use*; D008297:Male; D018782:Maze Learning / Q000502:physiology; D051379:Mice; D011597:Psychomotor Performance / Q000187:drug effects
D014151:Anti-Anxiety Agents; D044950:Flavanones; D003975:Diazepam