Due to the lack of highly selective dopamine D(1) or D(5) receptor ligands, only few data about activation or blocking of these receptor subtypes are available. The present review collects the available information about molecules with notable affinity for D(5) receptor subtype with the purpose to help the researchers to design novel D(5) selective ligands, whose discovery may enrich the knowledge about the physiological function of such a receptor, provide information about its topography, as well as lead to novel potential therapeutic tools.