The new compound HF-2159 (2-chloro-ll-(4'-methyl)piperazino-dibenzo-[b,f] [1,4]-thiazepine) studied in this paper in comparison with chlorpromazine shows the following properties: 1. Inhibition of motor drive, as manifested in the locomotor activity of mice and in the ‘open field’ test with rats. Its effectiveness here is respectively six and sixteen times greater than that of chlorpromazine. In both species of animals HF-2159 is only half as toxic as chlorpromazine. 2. Cataleptic action, which in rats is more than five times as strong as that of chlorpromazine. 3. Inhibition of apomorphine—induced gnawing in rats, an effect roughly thirty times as intense as that of chlorpromazine. 4. Temperature-lowering action in rats and rabbits, in the same range as that exerted by chlorpromazine. 5. Inhibition of the electrographic arousal reaction elicited by stimulation of the mesencephalic reticular formation, of an intensity not otherwise encountered in neuroleptic drugs with strong cataleptic activity. 6. Further, HF-2159 relaxes decerebration rigidity in cats, and is active in the usual analgesia tests. 7. HF-2159 has only slight and transitory effects on circulation, and no notable action on the autonomie nervous system (pupillary size, salivation, heart rate, bowel function). On the basis of the present pharmacological results, the compound may be expected to exert a neuroleptic effect in clinical use.
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