The present invention relates to novel steroid derivatives that ace on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex as well as methods for making the same and their applications to induce anesthesia, in the treatment of stress, anxiety, PMS, PND, and seizures such as those caused by epilepsy, to ameliorate or prevent the attacks of anxiety, muscle tension, and depression common with patients suffering from central nervous system abnormalities. The present invention comprises a compound represented by Formula (I): wherein, R, R1, R2, R3, R4, R5 are defined in the description of the invention. The present invention also includes formulations which consist of one or more of the compounds of Formula (I).