Presentation: 3A01

For the past 30 years clinically successful calcium channel blockers have selectively targeted L-type channels implicated in cardiovascular disease and migraine. More recent work suggests that other calcium channel subtypes, especially the N- and T-types, might provide strong candidates as therapeutic targets for a number of disorders including chronic/neuropathic pain, epilepsy, drug and alcohol addiction, neuroprotection, mood disorders and certain cancers. A major objective of all voltage-gated ion channel screening efforts is to balance drug efficacy with safety and tolerability. As N- and T-type calcium channels are involved in a number of critical normal physiological processes, successful drug development is likely to require the identification of selective state- and/or use-dependent blockers. The presentation will discuss recent efforts to develop rationale drug design strategies combined with electrophysiological screening (both manual and automated) to identify high affinity and selective state-dependent blockers of the N-type and T-type calcium channels.

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