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How effectively the brain can respond to injury and undergo structural repair has become one of the most exciting areas of contemporary basic and translational neuroscience research. Although there are no clinical treatments yet available to enhance repair of the damaged brain, there are a number of potential therapies being investigated. New drugs are designed to provide some degree of neuroprotection by preventing injured or vulnerable nerve cells from dying, or they are given in the hope of stimulating regenerative processes that could lead to the restoration or the formation of new connections that were lost because of the injury.The developments in pharmacology are based primarily upon understanding the molecular mechanisms of drug actions at the level of the genome or with respect to cellular metabolism. Although there is a substantial interest in the pharmacology of brain repair, there seems to be less concern with the various theories of central nervous system plasticity, organization, and reorganization after an injury.This review discusses some of the older and current ideas and theories that have been presented over the years to explain recovery of function. We then provide an overview of what is being done in the laboratory to develop new and safe drugs for the treatment of traumatic brain injuries.