The bed nucleus of the stria terminalis (BNST) regulates not only stress-related behaviors but also maternal behavior, pain-related behaviors, and reward-driven behavior. Dysfunction of the BNST leads to physiopathological states like anxiety disorder, post-traumatic syndrome disorder, anorexia, or addiction. Thus, a better understanding of the BNST emerges as an important challenge in order to develop innovative therapeutic strategies. Indeed, to improve our knowledge on the BNST, we first need to understand what shapes its activity. The BNST is strongly innervated by multiple inputs (glutamatergic, GABAergic, noradrenergic, dopaminergic, serotoninergic) giving rise to a part of its complexity. Importantly, under specific conditions (stress exposure, drug-withdrawal), endocannabinoid and neuropeptides can orchestrate the activity of the BNST. Here, we give a brief overview of the main pharmacological approaches targeting the BNST to assess the function of classical neurotransmitters and neuromodulators, from a pharmacological point of view through to behavior. © 2016, Springer International Publishing AG.