New approaches to the development of insect control agents have been revealed through the molecular description of neuropeptides, their biogenesis, action, and degradation. Prerequisite to the exploitation of a neuropeptide as a lead to control agent development is a thorough understanding of the biochemistry of the neuropeptide and appreciation of its physiological impact. Reliable bioassays must be coupled with advanced biochemical and molecular genetic technologies to overcome limitations imposed by the typically low endogenous levels of individual neuropeptides. Purification, amino acid sequencing, and gene cloning provide the molecular tools necessary for studies on neuropeptide synthesis, processing, secretion, receptor binding, and inactivation. Each of these areas consists of a number of amino acid sequence-, and enzyme-dependent steps which may be considered as targets for the development of highly specific control agents. These agents will include antagonists and superagonists, peptidomimetics, recombinant peptides delivered through the baculovirus technology, receptor blockers, and enzyme inhibitors.