Abstract: lucose is the main energy source in the central neuronal system. The family of facilitative glucose transporter proteins (GLUTs) is responsible for entry of glucose into brain. 13 members of the GLUTs family have been described thus far. Based on sequence similarities, the GLUTs family is divided into three classes, the first class (GLUT1-GLUT4) mostly transporting glucose; the second class (GLUT5, GLUT7, GLUT9 and GLUT11) mainly delivering fructose; the third class(GLUT6, GLUT8, GLUT10, GLUT12 and HMIT), however its function is still unclear. GLUT1 isomers are expressed in many kinds of cells, however，45kDa GLUT1 is the major transport protein mediating glucose across the blood brain barriers. The change of GLUT1 expression and function in some central nervous system diseases results in glucose transport process disturbed or glucose metabolism dysfunction. Recent researches show that GLUT1 can transport prodrugs by glycosylation modification across blood brain barrier. Therefore, method of glucose transport depending on GLUT1 may be a selective drug-delivery system. By utilizing such highly specific transport mechanism, it will widely attract the attention of researchers.