Authors: Mezler M, Hermann D, Swensen AM, Draguhn A, Terstappen GC, Gross G, Schoemaker H, Freiberg G, Pratt S, Gopalakrishnan SM, Nimmrich V
Abstract
Dysfunction of P/Q-type calcium channels is thought to underlie a variety of neurological diseases. There is evidence that migraine, Alzheimer´s disease, and epilepsy involve a gain-of-function of the channel, leading to abnormal presynaptic vesicle release. P/Q-channel blockers may normalize current flow and consequently lead to an alleviation of disease symptoms. Although the medical need is high, there are no such compounds on the market. Here we describe a high-throughput screen for P/Q-type calcium channel blockers and the confirmation of hits by automated electrophysiology. We generated a HEK293 cell line stably expressing the...

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