A polyamine agmatine is produced through decarboxylation of L -arginine by the enzyme arginine decarboxylase and is a new neurotransmitter in central nervous system (CNS). It has been suggested that agmatine has analgesic, anxiolytic and antidepressant activities in animals. In experimental studies, it also generates some favorable effects on cerebral damages and withdrawal syndromes involved in addictive drugs. Furthermore, it modulates some processes of learning and memory. Thus, agmatine may be an important target for the treatment of CNS disorders. However, the abnormal release and transmission of agmatine in brain may also be related to some CNS disorders, such as schizophrenia. Interaction of agmatine with other central neurotransmitter systems, such as the glutamatergic and nitrergic systems, seems to be very important. According to the current literature, we can expect that the central agmatinergic system may be a new key target in development of novel approaches for understanding the etiopathogenesis of CNS disorders and their treatment with drugs. The main goal of this article is to evaluate the effects of agmatine in CNS and underline its pharmacological actions in CNS and drug development.