Pharmacological properties of gamma-animobutyric acid and it derivatives. IV. Aryl gaba derivatives and their respective lactams.
Pharmacological properties of alpha-(AFG), beta-(FG) and gamma-(GFM) phenyl-substituted derivatives of GABA and their respective lactams (FP, FL, FM) were studied in rats and mice. All studied compounds diminished spontaneous and pharmacologically potentiated motility, lowered body temperature of mice, and weakened conditioned reflexes in rats. Some of the compounds (AFG, FG, FP) diminished activity of rats in the open-field test and symptoms of amphetamine- (AFG, FG, FP, FL, FM) and apomorphine-induced stereotypy (FL, FG). FG evoked catalepsy and potentiated chlorpromazine catalepsy in mice. The compounds potentiated action of narcotic and subthreshold doses of barbiturates and ethanol, had analgesic properties, and potentiated analgesic action of morphine. The most active and least toxic compound was beta-phenyl-gamma-aminobutyric acid (FG).
D000613:Aminobutyrates / Q000031:analogs & derivatives*; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D006801:Humans; D007769:Lactams / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009043:Motor Activity / Q000187:drug effects; D013239:Stereotyped Behavior / Q000187:drug effects; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity
D000613:Aminobutyrates; D007769:Lactams; D005680:gamma-Aminobutyric Acid