Currently, major controlling tools for insect pests depend on conventional chemical insecticides and genetically-modified organisms. These methods target neuro-synapses, channels and/or receptors that result in neurotoxicity or physiological imbalance. Unfortunately, this mode of action affects non-target animals and difficult to control insect species-specific. The application of classic insecticides is more and more restricted due to many problematic side effects, such as human and environmental toxicity, non-target insect and animal effects, and resistance. During the past decades new genomics/proteomics technologies such as RNA interference (RNAi), allow development of new classes and/or mode of action of insecticides and functionally screen bioactive compounds. Insect neuropeptides are the largest group, more than 90%, of all insect hormones that are involved in almost all physiological functions during the developmental and adult stages. Therefore, insect neuropeptide hormones and their receptors are good targets for discovery of insecticides such as RNAi and bioactive agents. In the presentation, insect case studies using neuropeptides and receptors suggest the possibility of novel biologically-based insect pest control methods.