The pathophysiology of anorexia nervosa (AN) is complex and involves alterations of serotonin, dopamine and histamine neurotransmitters. In addition, receptor activity is disturbed, presumably in response to the neurotransmitter changes. These alterations are reviewed in relation to symptomatology and outcome of AN. Neuropeptide and peripheral orexigenic and satiety peptide research is in its infancy but holds much promise to shed light on the pathophysiological mechanisms involved in this illness. Current drug therapies have not demonstrated the efficacy desired in the treatment of AN. Current therapies are reviewed and new drug targets are explored. Compounds that interact with serotonin, histamine and dopamine receptors may offer unique treatment opportunities. In the future, the manipulation of peptides may add to the therapeutic potential of pharmacotherapy.