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The concept of nootropics was introduced into pharmacology in the early 1970s by Corneliu Giurgea, a Belgian pharmacologist of Romanian origin, based on the study of 2-oxo-1-pyrrolidine derivatives, which later became known as racetams. The paper substantiates the position that the emergence of modern ideas about nootropics and similar compounds (psychoenergizers, antihypoxants, actoprotectors) in a certain sense was preceded by the concept of adaptogens by N.V. Lazarev (1953–1958), whose theoretical development went towards concretization of certain provisions of this concept. The formation of the problem of nootropics, their place in modern pharmacology, the origins and prospects for the development of the concept, the search for new pharmacological agents with nootropic properties are considered. Nootropic activity is analyzed from the standpoint of the mechanisms of action of racetams, neuropeptides, GABA derivatives, benzimidadols.