NS 1619 activates BKCa channel activity in rat cortical neurones

doi:10.1016/0014-2999(95)00251-F

European Journal of Pharmacology

Volume 280, Issue 2, 4 July 1995, Pages 215-219

https://doi.org/10.1016/0014-2999(95)00251-F Get rights and content

Abstract

Single channel recordings of large conductance Ca²⁺-activated K⁺ (BK_Ca) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BK_Ca channel activity in excised patches. In contrast, NS 1619 (1-(2′-hydroxy-5′-trifluoromethylphenyl)-5-trifluoromethyl-2(3H)benzimidazalone) induced concentration-dependent activation of BK_Ca channels with a calculated EC₅₀ of 32 μM. The NS 1619-induced activity was dependent on the presence of free Ca²⁺ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BK_Ca activity per se but prevented NS 1619-mediated activation.

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Short communicationNS 1619 activates BKCa channel activity in rat cortical neurones

Abstract

Trends. Pharmacol. Sci.

Eur. J. Pharmacol.

Eur. J. Pharmacol.

Activation of large conductance calcium-activated K+ channel by pinacidil in human pregnant myometrium

Br. J. Pharmacol.

The pharmacology of ATP-sensitive potassium channels

Annu. Rev. Pharmacol. Toxicol.

Ion channel modulation by NS 1619, the putative BKCa channel opener, in vascular smooth muscle

Br. J. Pharmacol.

Calculator programs for computing the composition of the solutions containing multiple metal and ligands used for experiments in skinned muscle cells

J. Physiol. (Paris)

Short communication
NS 1619 activates BK_Ca channel activity in rat cortical neurones

Activation of large conductance calcium-activated K⁺ channel by pinacidil in human pregnant myometrium

Ion channel modulation by NS 1619, the putative BK_Ca channel opener, in vascular smooth muscle