Neuropeptides represent the largest single class of signal compounds and are involved in regulation of development, growth, reproduction, metabolism and behavior of insects. Over the last few years there has been a tremendous increase in our knowledge of neuropeptide signaling due to genome sequencing, peptidomics, gene micro arrays, receptor characterization and targeted gene interference combined with physiological and behavior analysis. In this chapter we review the current knowledge of structure and distribution of insect neuropeptides and their receptors, as well as their diverse functions. We also discuss peptide biosynthesis, processing and expression, as well as classification of insect neuropeptides. Special attention is paid to the role insect neuropeptides play as potential targets for pest management and as a basis for development of insect control agents employing the rational/structural design approaches.