The Pharmaceutical Journal
Vol 280 No 7490 p207
23 February 2008

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Fatigue from “leaky” calcium channels

Restoring “leaky” calcium channels in muscle tissue reduces exercise-induced fatigue (Proceedings of the National Academy of Sciences 2008;105:2198).

Researchers found that during strenuous exercise in mice and humans, the major calcium channel required for excitation-contraction coupling in skeletal muscle was depleted of its calstabin-1 subunit and became leaky. In mice this led to decreased exercise tolerance.

However, administration of a calcium channel stabiliser, the 1,4-benzothiazepine derivative S107, prevented calcium channels becoming leaky, improved exercise capacity and may also protect against muscle damage.