6-(4-methyl-1-piperazinyl)morphanthridine (perlapine), a new tricyclic compound with sedative and sleep-promoting properties

Pharmacological studies of perlapine, a new dibenzoheteroepine derivative, have shown that its most prominent effects are depression of motor activity, central muscle-relaxation, and an increase in the telencephalic sleep phase as demonstrated by the EEG of the rat.Perlapine, though structurally related to some of the antipsychotic neuroleptics, does not exhibit to any marked degree the effects characteristic of that class of agents. One effect which distinguishes perlapine from the potent antipsychotic neuroleptics and also from the benzodiazepines is its strong inhibitory action on the reticular formation. This effect is thought to be a major factor in the sleep-promoting action of the drug.Chronic (4-week) EEG-studies of perlapine in the rat provided no evidence to suggest the development of tolerance.It is concluded that the mechanism of action of perlapine differs from that of other sleep-promoting agents.U.S. Adopted Name and British Approved Name, Code Number: HUF-2333.