Abstract: γ-Aminobutyric acid (GABA) receptor (GABAR) is an important target of insecticides. Up to date, all the commercially available GABAR-targeting insecticides are GABAR noncompetitive antagonists (NCAs). Competitive antagonists (CAs) of GABARs are potential insecticides, as they have similar functions to NCAs but different binding sites and mechanisms of action. Both CAs and NCAs exhibited insecticidal activities. However, the CA-insecticides are still in the research stage at present. Here, we review the latest research progress of insect GABAR CAs in the recent decade and hope to attract the attention of pesticide researchers.