The plant is a rare example of an herb the hallucinogenic properties of which have only recently been discovered. While its cousins in the Convolvulaceae family, such as the Rivea corymbosa (Ololiuhqui) and Ipomoea violacea (Tlitliltzin) were used in shamanic rituals of Latin America for centuries, the Hawaiian baby woodrose was not traditionally recognised as a hallucinogen. Its properties were first brought to attention in the 1960s, despite the fact that the chemical composition of its seeds is near identical to those of the two species mentioned above, and in fact contain the highest concentration of psychoactive compounds in the entire family.

Traditional use of the plant in India usually employed the leaves and roots of the plants, which are not psychoactive, as antiseptic and anti-inflammatory drugs.

The psychedelic properties of the seeds became known mainly through their use in Hawaii, Haiti and Puerto Rico, where impoverished members of the population would consume the seeds, seeking a "cheap buzz" as an alternative to alcohol. A sample made its way to Albert Hofmann, the discoverer of LSD, who confirmed the effects and analysed its chemical composition.