Bombesin receptors are a family of G protein-coupled receptors (GPCRs) which consists of 3 mammalian subtypes: BB1, BB2, and BB3 receptors. Both BB1 and BB2 are activated by several natural ligands, including neuromedin B and gastrin-releasing peptide. BB3, however, is an orphan receptor and has no known natural ligand. BB1 and BB2 agonists can stimulate tissue growth and muscle contraction, and also have an effect on the central nervous system. Although the exact role of BB3 is currently unknown, recent studies show a connection to insulin and body temperature regulation. Bombesin receptors could have a major impact in the treatment and detection of human cancers, CNS and behavioral disorders, obesity, and inflammatory conditions like sepsis and arthritis.