In a search for more environmentally benign alternatives to chemical pesticides, insect neuropeptides have been suggested as ideal candidates. Neuropeptides are neuromodulators and/or neurohormones that regulate most major physiological and behavioral processes in insects. The major neuropeptide structures have been identified through peptide purification in insects (peptidomics) and insect genome projects. Neuropeptide receptors have been identified and characterized in Drosophila and similar receptors are being targeted in other insects considered to be economically detrimental pests in agriculture and forestry. Defining neuropeptide action in different insect systems has been more challenging and as a consequence, identifying unique targets for potential pest control is also a challenge. In this chapter, neuropeptide biosynthesis as well as select physiological processes are examined with a view to pest control targets. The application of molecular techniques to transform insects with neuropeptide or neuropeptide receptor genes, or knockout genes to identify potential pest control targets, is a relatively new area that offers promise to insect control. Insect immune systems may also be manipulated through neuropeptides which may aid in compromising the insects ability to defend against foreign invasion.