NS 004—an activator of Ca2dependent Kchannels in cerebellar granule cells

Autor: Olesen, Søren-Peter, Munch, Ellen, Wätjen, Frank, Drejer, Jørgen
Zdroj: NeuroReport; April 1994, Vol. 5 Issue: 8 p1001-1004, 4p
Abstrakt: THE large-conductance Ca2-dependent Kchannels or BK channels in cerebellar granule cells were studied by patch-clamp technique, and the effects on channel activity of the molecule NS 004 (1-(2-hydroxy-5-chlorophenyl)-5-trifluoromethyl-2-benzimidazolone) were investigated. The channels had a unit conductance of 187 pS, were blocked by charybdotoxin and activated by internal Ca2. NS 004 (10–30 μM) significantly increased the single channel opening frequency as well as the mean open time. In whole-cell recordings the compound shifted the BK current-voltage relationship by up to 40 mV towards negative membrane potentials. NS 004 is an efficient BK channel opener, which may represent a novel approach to relaxation of neuronal cells expressing this type of Kchannel.
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