Insect neuropeptides are involved in almost all physiological processes in insects, such as diuresis, ecdysis, pheromone biosynthesis and control of muscle activity. Thus, these small peptide hormones and their receptors are promising targets for a novel generation of selective and non-neurotoxic insecticides. However, due to poor bioavailability, pharmacokinetics and short half-life the peptides themselves cannot be used as insect control agents. The past two decades have seen an increase in research into the discovery of non-peptide small molecules that function as mimics for neuropeptides. This review presents an overview on structure-activity studies, conformational analyses and peptidomimetic modifications of selected insect neuropeptides with a special potential for application in pest control.