The venoms of predatory cone snails represent a rich combinatorial-like library of evolutionarily selected, neuropharmacologically active peptides. A major fraction of the venom components are conotoxins——small, disulfide-rich peptides that potently and specifically interfere with neurotransmission by targeting a variety of proteins expressed on the cell surface, such as the ion channels of Ca²⁺, Na⁺ and K⁺, and the receptors of acetylcholine, 5-hydroxy tryptamine, NMDA, vasopressin and neurotensin. Because of low molecular mass, diversity of structure and targets, high specifiticy and tissue selectivity of conotoxins, they have more advantages over other naturally occurring toxins. Conopeptides could be also used as tools in neuroscience or as therapeutic agents. The conopeptides characterized to date are estimated to represent only 0.1% of the total present in 500 known species of Conus, therefore many novel conotoxins remain to be elucidated and explored. Pharmaceutical companies are now utilizing Conus-derived peptides to develop novel medications for pain, epilepsy and other disorders.