Background　General anesthetics produce widespread depression in the central nervous system by enhancing inhibitory neurotransmission and reducing excitatory neurotransmission. Excitatory neurotransmitters induce depolarization， such as glutamate and acetylcholine（ACh）. Whereas inhibitory neurotransmitters reduce postsynaptic activity by hyperpolarization or shunting excitatory currents， such as γ-aminobutyric acid（GABA） and glycine.　Objective　To investigate the mechanisms of drug molecular targets in general anesthesia.　Content　In this review， we briefly introduce the research progress of drug molecular targets of general anesthesia.　Trend　Studies on the contributions of anesthetic targets to general anesthesia may facilitate the development of more effective and safer anesthetics.