Pemoline (pemolina) was first synthesized in 1913 but its activity was not discovered until the 1930s. Under the names Betanamin, Cylert, Tradon, and Ceractiv it was used as a medication to treat attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Under the Convention on Psychotropic Substances, it is a Schedule IV drug. It is no longer generally available in the United States. Pemoline Magnesium, a chelate between pemoline and magnesium, displays certain pharmacological advantages over pemoline. The compound is the monohydrate of an equimolar mixture between pemoline and magnesium hydroxide. The absorption of pemoline magnesium is more rapid and the duration of action is extended, and the effect is more reliable.

Unlike other psychostimulants which are dopaminergic, pemoline is thought to be dopamimetic in nature. Pemoline passes the blood brain barrier and acts a surrogate for dopamine, not effecting endogenous intracellular dopamine. For this reason, and the fact that it has little or no affinity for adrenaline receptors, pemoline has minimal sympathomimetic side effects such as: dry mouth, reduction in appetite, high blood pressure, increased heart rate, constriction of smooth muscle, cardiac stress, dilated pupils and insomnia. There is some data to suggest that pemoline is a nootropic acting as a catalyst conductor in the synapses of the brain's memory centers, raising the efficiency of memory and assisting RNA formation in the brain. While drugs like Adderall and Ritalin are classified as Schedule II, pemoline is listed as Schedule IV (non-narcotic.) In studies conducted on primates, pemoline fails to demonstrate a potential for self-administration.