Valerian (Valeriana officinalis L.) is a perennial that has been used for medicinal purposes from the ancient times and valerian preparations including root and rhizome extracts are known to possess a variety of biological activities such as anticonvulsant, antidepressant, sleep aid, tranquilizer, and anti-HIV activities. Main components of the extracts were classified according to the structural features. Importantly, one of the main components, isovaleramide, has drawn our attention due to the concise structure, broad spectrum, and low toxicities. The general aspects including generation of this interesting molecule, a variety of activities, pharmacokinetic properties, derivatization, and fusion with other known drugs were described. Isovaleramide has been isolated from valerian probably as an isolation artifact after treatment of ammonia to prepare ammoniated tincture, and is known to exhibit anticonvulsant, anxiolytic, sedative, and sleep aid activities without distinct side effects such as excessive sedation and decreasing muscle tone. It was also found to be well absorbed into the circulation system without specific cytotoxicity and genotoxicity. The derivatives of isovaleramide, valpromide, valrocemide and valnoctamide were also briefly discussed.