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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

K+ channel openers activate brain sulfonylurea-sensitive K+ channels and block neurosecretion.

Vascular K+ channel openers such as cromakalim, nicorandil, and pinacidil potently stimulate 86Rb+ efflux from slices of substantia nigra. This 86Rb+ efflux is blocked by antidiabetic sulfonylureas, which are known to be potent and specific blockers of ATP-regulated K+ channels in pancreatic beta cells, cardiac cells, and smooth muscle cells. K0.5, the half-maximal effect of the enantiomer (-)-cromakalim, is as low as 10 nM, whereas K0.5 for nicorandil is 100 nM. These two compounds appear to have a much higher affinity for nerve cells than for smooth muscle cells. Openers of sulfonylurea-sensitive K+ channels lead to inhibition of gamma-aminobutyric acid release. There is an excellent relationship between potency to activate 86Rb+ efflux and potency to inhibit neurotransmitter release.[1]


  1. K+ channel openers activate brain sulfonylurea-sensitive K+ channels and block neurosecretion. Schmid-Antomarchi, H., Amoroso, S., Fosset, M., Lazdunski, M. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
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