Calcium enters the cytoplasm mainly via voltage-activated calcium channels (VACC), and this represents a key step in the regulation of a variety of cellular processes. Advances in the fields of molecular biology, pharmacology and electrophysiology have led to the identification of several types of VACC (referred to as T-, N-, L-, P/Q- and K-types). In addition to possessing distinctive structural and functional characteristics, many of these types of calcium channels exhibit differential sensitivities to pharmacological agents. In recent years a large number of toxins, mainly small peptides, have been purified from the venom of predatory marine cone snails and spiders. Many of these toxins have specific actions on ion channels and neurotransmitter receptors, and the toxins have been used as powerful tools in neuroscience research. Some of them (omega-conotoxins, omega-agatoxins) specifically recognize and block certain types of VACC. They have common structural backbones and some been synthesized with identical potency as the natural ones. Natural, synthetic and labeled calcium channel toxins have contributed to the understanding of the diversity of the neuronal calcium channels and their function. In particular, the toxins have been useful in the study of the role of different types of calcium channels on the process of neurotransmitter release. Neuronal calcium channel toxins may develop into powerful tools for diagnosis and treatment of neurological diseases. (C) 1997 Elsevier Science Ltd.