Octoclothepin, 8-chloro-1-(4-methylpiperazino)-10,11-dihydrodibenzo (b,f) thiepin, is a very potent
neuroleptic drug with pronounced central antidopaminergic and antiserotonin actions. In most animal experiments, its plharmacological profile resembles that of
perphenazine. Octoclothepin reveals an intensive central depressant action in a series of observational and instrumental procedures in rodents. Its active oral doses are within the range of 0.54 to 2.2 mg kg-1 in mice and of 0.1 to 4.8 mg kg-1 in rats. Octoclothepin possesses high cataleptogenic and anti-
apomorphine activities in rats; it is able to exert full protection against
apomorphine-induced
emesis in dogs after the dose of 0.1 mg kg-1 s.c. Octoclothepin reduces some actions and toxicity of d,
l-amphetamine and
phenmetrazine in rodents. In the rat corpus striatum, octoclothepin in doses of 0.5 and d1.5 mg kg-1 s.c. reduces the DA level and raises the HVA and
DOPAC levels significantly. Octoclothepin has
antihistamine, antiserotonin and antianaphylactoid actions, it exhibits a high protection against the lethal action of
adrenaline and
noradrenaline in mice and rats, respectively. Acute toxicological data in mice, rats, rabbits and dogs are given. Clinical
antipsychotic effectiveness of octoclothepin has been verified in a large population of psychiatric patients.