ns-309 and benzimidazol-2-one

We have identified and characterized the compound NS309 (6,7-dichloro-1H-indole-2,3-dione 3-oxime) as a potent activator of human Ca2+ -activated K+ channels of SK and IK types, whereas it is devoid of effect on BK type channels. IK- and SK-channels have previously been reported to be activated by the benzimidazolinone, 1-EBIO and more potently by its dichloronated-analogue, DC-EBIO. NS309 is at least 1000 times more potent than 1-EBIO and at least 30 times more potent than DC-EBIO when the compounds are compared on the same cell.

Topics: Benzimidazoles; Calcium Channel Agonists; Cell Line; Dose-Response Relationship, Drug; Humans; Indoles; Intermediate-Conductance Calcium-Activated Potassium Channels; Kinetics; Oximes; Patch-Clamp Techniques; Potassium Channels, Calcium-Activated; Small-Conductance Calcium-Activated Potassium Channels