The paper is devoted to the role of GABA system in the pharmacotherapy of ischemic brain injuries. In an analysis of the neuroprotector activity of GABA-mimetics, both their involvement in the maintenance of a balance between exciting and inhibiting processes and participation of the GABAergic mechanisms in regulation of the cerebrovascular tone are considered because proper blood supply is an important factor in the successful therapy of patients with ischemic brain injuries. Data available in the literature and the results of original investigations are summarized to assess the cerebrovascular and neuroprotector properties of GABA, as well as agonists and modulators of GABA receptors (muscimol, picamilon, phelbamate, clomethiazole, etc.). Particular attention is given to the neutroprotector and cerebrovascular activity of a new drug composition GABA-mimetic pirrolidone and pyroglutamic acid. This drug is capable of improving the cerebral blood supply, limiting the zone of ischemic injury, preventing an increase in the level of lactate and lipid peroxidation products, modifying nitric oxide content, and restoring the psychoneurological status of experimental animals with ischemic brain injury models.