We tested the effects of roasted and non-roasted Zizyphi Spinosi Semen (ZSS) hot water extracts on pentobarbital-induced sleeping behavior, pentylentetrazole-induced convulsions, and locomotor activity in mice. Both ZSS extracts decreased locomotor activity and pentylentetrazole-induced convulsions. Both extracts alos dose-dependently shortened the sleep onset and prolonged the sleep time induced by pentobarbital, with roasted extract being more potent. In addition, chemical constituents in HPLC also were different. Thus, both roasted and non-roasted ZSS extracts potentiate the sleep onset and the sleeping time induced by pentobarbital, decrease locomotor activity, and reduce pentylentetrazole-induced convulsions, with roasting improving extract potency.