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Significance Large-conductance Ca2+ -activated K+ (BK) calcium-activated potassium channels alter the excitability of a wide variety of cells including nerves and muscle. These channels are potential targets to treat diseases such as overactive bladder, hypertension, and erectile dysfunction. We have shown that a novel compound called GoSlo opens these channels and this effect is blocked when three mutations are introduced. The identification of this potential interaction site may permit the development of more potent, efficacious BK channel modulators to help treat the above diseases.

Molecular mechanisms underlying the effect of the novel BK channel opener GoSlo: Involvement of the S4/S5 linker and the S6 segment