In this review, the development of understanding of the biological functions of carnosine is briefly discussed. Carnosine was first described as a component of meat in 1900 by V. S. Gulevitch. Changes in the concepts of the role of carnosine in metabolism are followed starting from the early suggestion that it is the end product of protein degradation to the modern ideas based on demonstrating its specific involvement in intracellular signaling regulation in excitable tissue cells. The discovery of the ability of carnosine to regulate expression of early response genes broadens the concept about carnosine as a cellular peptide regulator. The first attempts for application of carnosine in sport and medical practice are described.