[1] It was originally identified in 1932 in plant alkaloid extracts[2] and has been isolated from Dicentra cucullaria, Adlumia fungosa, and several Corydalis species (all in subfamily Fumarioideae, previously known as family Fumariaceae).

This property is utilized in laboratories around the world in the in vitro study of epilepsy, generally in hippocampal or cortical neurons in prepared brain slices from rodents.

This compound is also routinely used to isolate glutamatergic (excitatory amino acid) receptor function.

[citation needed] In addition to being a potent GABAA receptor antagonist, bicuculline can be used to block Ca2+-activated potassium channels.

[3] Sensitivity to bicuculline is defined by IUPHAR as a major criterion in the definition of GABAA receptors