The aim of this review was the discussion of creatine involvement in metabolism of nervous tissue cells. The questions of creatine penetration through the blood brain barrier and creatine transporter expression were raised. Also mechanisms of creatine protective effect were considered at experimental models of brain ischemia. It was shown that creatine was involved in energy metabolism (creatine phosphate synthesis), inhibition of excitotoxicity. Besides it had antioxidant and antiproliferative effects. The creatine delivery problem was also discussed. Synthesis of substances capable to get through the blood brain barrier without CRT was the possible solution of the problem. The most perspective substances were creatine amides apparently capable to move through cell membranes without amino acid transporters. Prospects of their application were discussed.