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Toxicol Lett. 2005 Mar 15;155(3):421-6.

The fungal neurotoxin lolitrem B inhibits the function of human large conductance calcium-activated potassium channels.

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AgResearch Limited, Biomembrane Group, Grasslands Research Centre, Tennent Drive, Private Bag 11008, Palmerston North 5301, New Zealand.


The effects of the mycotoxin lolitrem B on the function of hSlo large conductance calcium-activated potassium channels expressed in HEK293 cells have been investigated using inside-out membrane patches. Lolitrem B potently inhibited hSlo potassium currents activated by depolarising voltage pulses in the presence of 10 microM free calcium. At a concentration of 100 nM, lolitrem B rapidly and completely inhibited outward potassium currents. The concentration that produced half-maximal inhibition was 3.7 nM, indicating a high apparent affinity for hSlo channels. This is the first time that a molecular site of action has been identified for a compound of the lolitrem structural class of indole diterpene and identifies a novel BK channel blocker.

[Indexed for MEDLINE]

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