Valerian flower extracts were used in perfumery since the 6th century. Employed as an anti-anxiety agent and sleep aid for more than 1,000 years, valerian is also used an antispasmodic in hysteria and other nervous disorders. Valerian was especially popular during World War I, when it was used to treat shell-shock. It possesses mild sedative and tranquillizing properties and is often prescribed with bromides or other sedatives. It is popularly used as a tea prepared from 2–3 g of the dried herb or equivalent amounts of tincture. Standardized mixtures of valepotriates containing dihydrovaltrate (80%), valtrate (15%) and acevaltrate (5%) are available in some countries. These materials are usually extracted from the roots of other species of valerian which produce higher amounts of valepotriates than V. officinalis.

The identity of the sedative components of the root was not ascertained for a long time due to the unstable nature of the active constituents and genetic variability of the plant material. Though valepotriates were thought to be the sedative components, presence of valerenone, a sesquiterpene component of the volatile oil in N. jatamansii used as a popular sedative in Ayurveda led to further activity testing. Japanese researchers concluded that the sedative property was due to the sesquitepene components of the volatile oil. Further valepotriates are reported to be toxic in vitro.