a-Acetylbutyrolacone was used as an intermediate for the development of the non-nucleoside human immunodeficiency virus inhibitors and for the synthesis of antitumor agent which has thymidylate synthase (TS) and dihydrofolate reductase (DHFR) properties. Moreover, it has been characterized for use as a fluorogenic reagent for the spectrofluorimetric determination of primary amines.

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.