Calcium channel antagonists: Past and future

The calcium channel antagonists are a chemically heterogeneous group of agents that have served both as therapeutic agents for discrete cardiovascular diseases, notably hypertension, and as molecular tools with which to investigate calcium channel structure and function over the past two decades. They owe both of these activities to their selective interaction with one particular class of channel - the L-type voltage-gated calcium channel. Their future role as therapeutic agents may be modified by the results from the ALLHAT trial that indicated diuretics as the initial stage of therapy. Their powerful interactions with one class of channel has spurred the search for similar small molecule synthetic drugs active at other classes of voltage-gated calcium channels. Such agents are potentially of use in a variety of CNS disorders: thus far, this search has not met with significant therapeutic success.