Insect neuropeptides play a vital role in chemical communication between cells, and consequently in growth, metabolism and behavior. The insect neuropeptide SIFamide (SIFa) is a short peptide comprised of 10-15 amino acid residues with a conserved ‘-SIFamide’ motif at the carboxyl terminus. SIFa is mainly secreted from the four pars intercerebralis neurons of brain, and is involved in the regulation of courtship, sleep and feeding behaviors via activation of the specific G protein-coupled receptor (SIFa receptor, SIFaR). Here, we summarize progress in research on the structural characteristics and physiological functions of SIFa and its receptor, and review the prospects of developing specific pesticides targeting the SIFa/SIFaR pathway to control important insect pests.