Endogenous opioids and μ-opioid receptors (MORs) have long been implicated in the mechanism of appetite control and, in particular, hedonic processes associated with food evaluation, consumption and orosensory reward processes. In animal models of binge eating, selective MOR antagonists suppress food consumption. In humans, non-selective opioid receptor antagonists reduce hedonic taste preferences and food intake, particularly for palatable foods, and cause short-term weight loss. These effects have been linked to direct stimulation of MORs and modulation of dopamine release within the reward circuitry including the nucleus accumbens. These findings suggest that reduction of MOR-mediated hedonic and motivation processes driving consumption of highly palatable foods may be a promising therapeutic approach and provide a strong rationale for developing safer and more selective MOR antagonists or inverse agonists for disorders of 'appetitive motivation' including obesity and binge-eating disorder.