Compositions and methods that act on Neuropeptide S receptors (NPSR) (also known as “TGR23” or “vasopressin receptor-related receptor 1 (VRR1)”) to cause desired effects in the bodies of human or animal subjects. Neuropeptide S (NPS) and other agonists of the NPSR may be administered to cause arousal, awakening, alertness, spontaneous movement, bronchoconstriction, contraction of bronchial smooth muscle or other effects. Antagonists of the NPSR may be administered to cause decreased arousal, decreased awakening, decreased alertness, decreased spontaneous movement, sleep, somnolence, sedation, anxiolytic effects, normalized sleep patterns, normalized sleep stages, increased duration of sleep, bronchodilation, relaxation of broncheal smooth muscle or other effects.