ABSTRACT
The anxiosedative properties of 2-hydroxyimino-3-indolylyl(aryl)-4-oxo-2,3,4,5,6,7-hexahydrobenzofuranon derivatives have been studied using the open-field test, elevated plus-maze test, and conflict drinking procedure as developed by Vogel. It is established that all derivatives with both indole and aryl substituents produce a sedative effect. However, an anxiolytic effect is determined by the presence of indole substituent in the third position of the hexahydrobenzofuran molecule.
Subject(s)
Anti-Anxiety Agents/pharmacology , Benzofurans/pharmacology , Hypnotics and Sedatives/pharmacology , Animals , Anti-Anxiety Agents/chemistry , Benzofurans/chemistry , Conflict, Psychological , Drinking Behavior/drug effects , Hypnotics and Sedatives/chemistry , Male , Maze Learning/drug effects , Motor Activity/drug effects , Rats , Rats, Wistar , Structure-Activity RelationshipABSTRACT
Fenotropil and its structural analog--compound RGPU-95 to a greater extent reduce the severity of anxious and depressive behavior in male rats than in females. On expression of the anxiolytic compound RGPU-95 significantly exceeds Fenotropil, but inferior to Diazepam; of antidepressant activity--comparable to Melipramin and exceeds Fenotropil.