Conotoxins are peptide toxins, ranging in size from 12 to 30 amino acids, isolated from the venom of snails from the Conus genus . Members of this peptide family target a range of membrane receptors with both high potency and selectivity and as a consequence are useful as neurological probes and have a range of potential pharmaceutical applications. A subfamily of conotoxins, the alpha-conotoxins, were believed to interact only with nicotinic acetylcholine receptors (nAChRs), which have been implicated in a range of disorders, including Alzheimers disease, schizophrenia, depression and small cell lung carcinoma and also play a role in analgesia and addiction . However, recently we showed that a subset of the alpha-conotoxins also modulate N-type calcium channels by acting as agonists of the G-protein-coupled GABAB receptor . GABAB receptors  are G-protein coupled receptors for gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter of the brain, and are a promising target for the treatment of a range of neurological and psychiatric disorders including pain, depression and drug addiction . One member of this conotoxin subset, Vc1.1, has now been developed as an orally active lead molecule for the treatment of neuropathic pain . This presentation will describe our discovery that certain alpha-conotoxins target the GABAB receptor, our efforts towards defining the molecular details of this interaction.