Abstract: Pregnanolone derivatives, substituted in 3 alpha-position with the cationic group, of general formula I, and a method of the production of these compounds and their utilization for treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post traumatic stress disorder, and other diseases related to stress, anxiety, schizophrenia, and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy, and gliomas. The compounds are also used for production of veterinary and human pharmaceutical preparation for treatment of above mentioned diseases and for production of pharmaceutical preparations containing these compounds.