Valproic acid is a well-known drug long used in neurology as an antiepileptic drug and in psychiatry because of its mood-stabilising effect. Various mechanisms of valproic acid activity have been described (through gamma-aminobutyric acid system – GABA, glutamatergic activity, monoamines, ion channels, gene expression modulation and others), resulting in a decrease of neuronal activity but also affecting other processes, such as apoptosis, inflammation and differentiation of neurons. A wide range of possible activity mechanisms enables the potential use of this “old drug” in new indications. One of the considered aspects of valproic acid activity is its neuroprotective effect, which has been noted so far both in the cellular and in the animal models. The aim of this article is to recapitulate current knowledge on the well-known and novel mechanisms of valproic acid activity in the context of its possible neuroprotective effect.