[Pharmacological investigations of 4'-fluoro-4-(4-methyl-peperidono)-butyrophenone with respect to its sedative and sleep-inducing properties (author's transl)].
The butyrophenone melperone (Eunerpan) in mice and rats caused a prominetn inhibition of spontaneous activity, whereas cataleptogenic and apomorphine-antagonistic properties were less pronounced. In rats the sleep-cycle was altered: decrease of wakefulness, increase of slow-wave sleep and a moderate reduction of rapid eye movement-(REM) sleep. In contrast to thioridazine and chlorpromazine the effect lasted only for 4 h, followed by a slight REM rebound. In rabbits melperone caused a decrease of muscle tone and with somewhat higher doses an inhibition of the arousal-reaction. As seen by the computerized spontaneous cortical EEG, dosages below 1 mg/kg caused a shift of the dominant frequency from theta- to delta-rhythm and an increase of power. Therefore the neuropharmacological pattern of the butyrophenone melperone is closely related to those of thioridazine or chlorpromazine, without, however, having their long action.
D000818:Animals; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001143:Arousal / Q000187:drug effects; D002090:Butyrophenones / Q000494:pharmacology*; D002746:Chlorpromazine / Q000494:pharmacology; D004569:Electroencephalography; D005260:Female; D006801:Humans; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009129:Muscle Tonus / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D012890:Sleep / Q000187:drug effects*; D012895:Sleep, REM / Q000187:drug effects; D013239:Stereotyped Behavior / Q000187:drug effects; D013881:Thioridazine / Q000494:pharmacology
D002090:Butyrophenones; D001058:Apomorphine; D013881:Thioridazine; D002746:Chlorpromazine
Pharmakologische Untersuchungen zur sedativen und schlafanstossenden Wirkung von (4'-Fluor-4(4-methylpiperidino)-butyrophenon (Melperon)