[Abstract ] Background The complex crystal structure of general anesthetics desflurane or propofol and pentameric ligand-gated ion channels(pLGICs ) in prokaryotic cell membrane, provides a novel structural framework for the design of general anesthetics and of allosteric modulators of brain pLGICs and gets many new experiment support about the allosteric regulation theory. Objective To summarize the general anesthetics molecular sites and allosteric regulation mechanism. Content This paper introduces the origin and development of the word "allosteric", expounds the molecular sites and modulate mechanisms of general anesthetics action on protein models and ion channels, and proposes two key binding sites of anesthetics in pLGICs mediating receptor affinity and direct activation receptor respectively. But the allosteric regulation is the main mechanism of mediating receptor affinity. Trend With the development of science and technology and application of many new technology and new method, it will gradually be understanded that various kinds of molecular sites of general anesthetics in the central nervous system and regulation mechanism.