In the current review, the data selectively scrutinized from the in vitro/in vivo studies about identifying anxiolytic molecular mechanisms of V. In addition to valerenic acid isovaleric acid, didrovaltrate, borneol, and some lignans have been also proposed to contribute to anxiolytic effect of the plant. Although modulation of gammaaminobutyric acid (GABA) receptors has been revealed to be the leading mechanism of the plant based on the existence of valerenic acid, several studies described interaction of valerenic acid with glutamergic receptors. Among them, valerenic acid is a marker compound for standardization of the root extracts of the plant and has been reported in many in vitro/in vivo studies to be responsible for anxiolytic action of the plant. pinoresinol, hydroxypinoresinol), alkaloids (e.g. valtrate, didrovaltrate, isovalerenic acid), sesquiterpenes (e.g. officinalis has a complex phytochemistry consisting of the esterified iridoid derivatives known as valepotriates (e.g. Its root extract is one of the most effective herbal sedatives and tranquilizers, where the plant is also used for treatment of gastrointestinal spasms. (Valerianaceae) is one of the most reputed ancient medicinal plants used in modern phytotherapy and traditional medicine.