Abstract: Urotensin II (UII) is the most potent vasoconstrictor among the identified vasoactive peptides. UII and its receptor (UT), which play varies of physiological roles, are widely expressed in central nerve system and peripheral organs. The change on the expressional level of UII/UT system has been proved to be closely correlated with pathological conditions. Therefore, UII/UT system was considered to be a potential target for treating many diseases. This review article is devoted to the latest research progress of UII/UT system in several aspects including ligand and receptor distribution, physiological activity, characteristics under pathological conditions and antagonist classification.