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. 2011 Jan 17;17(1):4–31. doi: 10.1111/j.1755-5949.2009.00116.x

Table 3.

Effects of riluzole on voltage‐gated and other K+ currents and channels

Current/channel Effect (%) Concentration (μM) Tissue Reference
Potassium currents
Fast 1 component Inhibition 21a Frog myelinated nerve fiber [58]
Fast 2 component Inhibition 24a Frog myelinated nerve fiber [58]
Slow component Inhibition 413a Frog myelinated nerve fiber [58]
Delayed rectifier K+ current Inhibition 88a Cultured embryonic rat cortical neurons [41]
Voltage‐gated potassium channels
Mouse Kv1.1 Inhibition 92a NIH/NT3 cells [47]
Mouse Kv1.3 Inhibition 50a NIH/NT3 cells [47]
Rat Kv1.5 Inhibition 40a CHO cells [64]
Kv1.5 Inhibition (30%) 100 Rat vascular smooth muscle [62]
Human Kv1.5 Inhibition 95a MEL cells [47]
Rat Kv3.1 Inhibition 124a CHO cells [64]
Human Kv3.1 Inhibition 95a HEK‐293 cells [47]
Rat Kv3.2 Inhibition 100a COS‐7 cells [47]
Kv1.4 Inhibition 70 Bovine adrenal zona fasiculata cells [61]
Rat Kv4.2 Inhibition 130a LTK cells [47]
Rat Kv4.3 Inhibition 116.5a CHO cells [63]
HERG Kv11.1 Inhibition 50a HEK‐293 cells [47]
Two pore potassium channels
TRAAK Activation (3.9 fold increase) 100 COS cells [72]
TREK‐1 Activation (∼2 fold increase) 100 COS cells [71]
TREK‐1 Activation 110b Not stated [47]
TREK‐1 Activation (3.3 fold increase) 100 Bovine adrenal zona fasciulata cells [74]
THIK‐1 Inhibition (36%) 500 Mouse cerebellar Purkinje neurons [75]
Calcium‐dependent potassium currents and channels
After hyperpolarization current No effect 10 Cultured embryonic rat spinal motor neurons [17]
After hyperpolarization current Potentiation (70%) 3 Rat hippocampal pyramidal neurons [16]
After hyperpolarizaton No effect (amplitude) 1 GH3 neuroendocrine cells [35]
Increase (four‐fold in recovery time)
BK KCa Activation 5b GH3 neuroendocrine cells [66]
BK KCa Activation (30%) 10 GH3 neuroendocrine cells [35]
BK KCa Activation (2 fold increase) 5 Human retinal pigment epithelial cells [67]
BK KCa Activation (2 fold increase) 10 Human skeletal muscle cells [50]
Human BK KCa1.1 Activation (2 fold increase) 100 HEK‐293 cells [47]
Human SK1 KCa2.1 Activation (250 nM Ca2+) 21b HEK‐293 cells [47]
Rat SK2 KCa2.2 Activation (250 nM Ca2+) 12.8b HEK‐293 cells [47]
Human SK3 KCa2.3 Activation (250 nM Ca2+) 12.5b COS‐7 cells [47]
Rat SK3 Activation (2.3 fold increase, 100 nM Ca2+) 3 HEK‐293 cells [68]
Human SK4 KCa3.1 Activation (250 nM Ca2+) 1.9b HEK‐293 cells [47]
Rat SK2 K(Ca) Activation (Ca2+ free) 43b HEK‐239 cells [16]
(100 nM Ca2+) 0.11b

aIC50.

bEC50.