2 (SK) channel negative modulator; inhibits SK channel currents (Kd
values are 0.42, 0.6 and 0.73 μ
M for SK1, SK2 and SK3 respectively at 0.5 μ
). Exhibits selectivity for SK channels over KCa
1.1 (BK), KCa
3.1 (IK), Kv
channels. Inhibits afterhyperpolarization in hippocampal slices.
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Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hip
Strøbaek et al.
Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators of small conductance Ca2+-activated K+ channels.
Negative gating modulation by (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine (NS8593) depends on residues in the inner pore vestibule: pharmacological evidence of deep-pore gating of KCa2 channels.
Jenkins et al.