This review summarizes current data and the results of the authors’ own investigations of the neurotropic, psychoactive, and analgesic properties of benzimidazole and its derivatives. Using a series of compounds of this class as a examples, different aspects of the actions of benzimidazoles on the nervous system of lab animals (mollusks, mice, rats, cats) are considered. The efficacy of benzimidazoles is shown to be due to actions on a number of important physiological mechanisms regulating the functional state of nerve cells and neurotransmitter systems, inflammation processes, and pain.