The central dopaminergic system plays a critical role in the reinforcing effects of nicotine, which are key determinants in the urge to smoke. Previous study has demonstrated that immediate administration of 10-mg aripiprazole significantly decreased various subjective responses to smoking. The present study investigated whether 2-week treatment with 10-mg aripiprazole could attenuate waking and postprandial urges to smoke in Chinese male and female heavy smokers. A randomized and placebo-controlled pilot clinical study was conducted to assess the effect of aripiprazole on various responses to smoking. The primary outcomes were subject's ratings on questionnaires of smoking urge, withdrawal syndromes, and cigarette evaluation. All participants were administered either placebo or 10-mg aripiprazole for 2 weeks. Throughout the experiment, participants were required to self-report (1) smoking urge and nicotine withdrawal symptoms before their first cigarette after awakening and after lunch and (2) subjective responses to the first cigarette smoked of the day and after lunch. Aripiprazole was associated with significantly decreased waking and postprandial urges to smoke. Aripiprazole failed to produce a significant effect on overall nicotine withdrawal symptoms after awakening and after lunch. However, waking, but not postprandial, withdrawal craving and syndromes were significantly reduced by aripiprazole. Aripiprazole had no effect on the overall subjective responses to the first cigarette of the day and after lunch. The attenuating effects of aripiprazole on waking and postprandial urges to smoke demonstrate the promising effect of aripiprazole in the treatment of nicotine dependence.