The generation of acupuncture effect is closely related to the structural integrity and normal function of nervous system. Neurotransmitters are the material basis for the generation of acupuncture effect. We reviewed the literature of neurobiological mechanism of acupuncture effect and summarized the regulatory mechanism of acupuncture on neurotransmitters under different body states. Neurotransmitters participate in the activation of acupuncture signals locally at acupoints, the transmission and integration of acupuncture information at the central level, and the regulation of diseases in effector organs. The regulation of neurotransmitters by acupuncture is closely related to the body state and has the characteristics of normalizing regulation effect. The acupuncture effect generated by neurotransmitters at acupoints is nonspecific. In a specific body state, neurotransmitters participate in the functional regulation of target organs and effector organs, reflecting the specific effect of acupuncture.