Recent brain imaging studies have shed light on understanding the pathogenesis of mood disorders. Evidence of structural, chemical, and functional brain changes, particularly in prefrontal cortex, cingulate, and amygdala, has been revealed in major depressive disorder (MDD). Furthermore, imaging techniques have been applied to monitor the effects of antidepressants (ADs) both in the brains of healthy volunteers and MDD patients. Although with some discrepancies due to the differences in study designs and patient samples, imaging findings have shown that ADs, particularly those having effects on the serotonergic system, modulate the volumes, functions and biochemistry of brain structures, i.e. dorsolateral prefrontal cortex, anterior cingulate and amygdala, which have been demonstrated abnormal in MDD by earlier imaging studies. This paper reviews imaging studies conducted in MDD patients and healthy controls treated with different ADs.