Abstract: Octopamine acts as a neurotransmitter, neurohormone or neuromodulator in the invertebrate nervous tissue, regulating several physiological processes in insects including feeding, locomotion and reproduction. The octopamine receptors mediate the physiological effects of octopamine by means of simulating the adenylate cyclase system and other second-messengers. Octopamine receptors are considered to be useful biorational targets for the development of potent, selective insecticides. This paper reviewed the research works on the biological effects, mechanism, pharmacological classification and molecular biology of octopaminergic receptors. Potential targets for designing new lead molecules acting on OA type system are discussed.