[Effects of a new psychotropic agent, CS-430, on the central nervous system of experimental animals (author's transl)].
In rats and rabbits with chronically implanted electrodes CS-430(10-bromo-2, 3, 7, 11b-tetrahydro--11b-(2-fluorophenyl)-oxazolo(3, 2d) [1, 4]benzodiazepine-6(5H)-one) (3 mg/kg, .o.) decreased the slightly awake period and increased the slow-wave sleep period. The onset time of sleep was significantly shortened. In the rat pre-treated with p-chlorophenylalaine (500 mg/kg, p.o.), the awake period was remarkable increased and the slow wave sleep period was considerably decreased at 48 hours after the pre-treatment. In these rats CS-430 given in the same dose decreased significantly the awake peiod and the onset time of sleep and increased the slow wave sleep period. CS-430 raised the threshold of the arousal response with stimulation of the posterior hypothalamus, but not of the mesencephalic reticular formation. These effects of CS-430 were almost as potent as those of nitrazepam (NZP). CS-430 reduced duration of after-discharges following stimulation of the hippocampus, depressed the decerebrate rigidity and inhibited activity of lumbar gamma-motoneurons in anesthetized cats. CS-430 (10 mg/kg, p.o.) inhibited the evoked responses recorded from the proreus gyrus following stimulation of either the baso-magnocellularis of the amygdaloid nuclear or the ventral hippocampus, although such did not inhibit the responses between the olfactory bulb and the pyriform cortex, the thalamus and the sensory-motor cortex. Thus CS-430 has a sleep-inducing effect in animals of almost the same potency as is seen with NZP, and site(s) of the action in the limbic system appear to be specific.
D000679:Amygdala / Q000187:drug effects; D000818:Animals; D001143:Arousal / Q000187:drug effects; D001570:Benzodiazepinones / Q000494:pharmacology*; D002415:Cats; D002490:Central Nervous System / Q000187:drug effects*; D003655:Decerebrate State; D004558:Electric Stimulation; D004569:Electroencephalography; D005071:Evoked Potentials / Q000187:drug effects; D005260:Female; D010134:Fenclonine / Q000037:antagonists & inhibitors; D006624:Hippocampus / Q000187:drug effects; D008297:Male; D009047:Motor Neurons, Gamma / Q000187:drug effects; D010080:Oxazoles / Q000494:pharmacology; D011619:Psychotropic Drugs / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D012890:Sleep / Q000187:drug effects
D001570:Benzodiazepinones; D010080:Oxazoles; D011619:Psychotropic Drugs; D010134:Fenclonine