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

Table 5.

Effects of riluzole on neurotransmission and ligand‐gated neurotransmitter receptors

Current/channel Effect (%) Concentration (μM) Tissue Reference
Excitatory neurotransmission and transmitter release
Evoked population spike and field EPSP Inhibition 5a Rat CA1 hippocampal neurons [89]
Evoked cortical field potential Inhibition 29.5a Rat cortex [13]
Evoked excitatory transmission Inhibition 6a Rat striatal neurons [12]
Evoked excitatory transmission Inhibition (45%) 10 Rat lumbar spinal cord interneurons and motor neurons [24]
Evoked glutamate EPSC amplitude Inhibition (8%) 0.5 Cultured neonatal rat hippocampal neurons [46, 93]
(33%) 10
(85%) 20
Excitatory miniature EPSCs No effect 10 Rat lumbar spinal cord interneurons and motor neurons [24]
Excitatory miniature EPSCs No effect 10 Neonatal rat hypoglossal motor neurons [27]
Release of [3H]glutamate Inhibition (77%) 19.5a Human, rat and mouse neocortex slices [88]
Release of [3H]dopamine Inhibition (72%) 6.8a Human, rat and mouse neocortex slices [88]
Release of [3H]dopamine Inhibition 1–10a Rat striatum synaptosomes [197]
Release of [3H]acetylcholine Inhibition (92%) 3.3a Human, rat and mouse neocortex slices [88]
Release of [3H]serotonin Inhibition (53%) 39.8a Human, rat and mouse neocortex slices [88]
Evoked glutamate EPSC amplitude Inhibition (11%) 1 Adult mouse hippocampal CA1 neurons [92]
Excitatory amino acid receptors
Glutamate‐elicited depolarization Inhibition (20%) 30 Rat striatal neurons [12]
(40%) 100
Glutamate‐elicited depolarization No effect 30 Rat cortical neurons [13]
Radioligand binding at glutamate receptors Inhibition (30%) 100 μM Rat brain [85]
Radioligand binding at glutamate receptors No effect 100 μM Rat brain [47]
Kainate‐elicited depolarization Inhibition 101a Cultured rat cortical neurons [97]
Kainate‐elicited depolarization No effect 20 Cultured neonatal rat hippocampal neurons [93]
Rat Kainate glutamate receptor Inhibition 167a Xenopus oocytes [95]
Radioligand binding at kainate glutamate receptors No effect 100 μM Rat brain [47]
Rat NMDA glutamate receptor Inhibition 18a Xenopus oocytes [95]
Radioligand binding at NMDA glutamate receptors No effect 100 μM Rat brain [47]
NMDA‐elicited depolarization No effect 20 Cultured neonatal rat hippocampal neurons [93]
Evoked NMDA glutamate receptor EPSC Inhibition (37%) 20 Cultured neonatal rat hippocampal neurons [93]
Inhibitory amino acid receptors
Radioligand binding at GABAA receptors No effect 100 μM Rat brain [85]
Rat GABAA receptors No effect 10 μM to 1 mM HEK‐293 cells [103]
Rat GABAA receptors Inhibition (54%, 1 mM GABA) 30 HEK‐293 cells [105]
Potentiation (2.3‐fold, 3 μM GABA) 30
GABAA receptor Potentiation 53b Cultured rat hippocampal neurons and oocytes [104]
Evoked GABA IPSC amplitude Inhibition (24%) 20 Cultured neonatal rat hippocampal neurons [93]
Radioligand binding at GABAB receptors No effect 100 μM Rat brain [85]
Evoked glycinergic IPSC Inhibition (87%) 10 Neonatal rat hypoglossal motor neurons [76]
Miniature glycinergic IPSC No effect 10 Neonatal rat hypoglossal motor neurons [76]
Rat glycine receptors No effect 30 μM to 1 mM HEK‐293 cells [103]
Radioligand binding at glycine receptors No effect 100 μM Rat brain [47, 85]
Other ligand‐gated neurotransmitter receptors
5‐HT3 receptor Inhibition 3.6a NCB‐20 neuroblastoma cells [106]
Human skeletal muscle nicotinic acetylcholine receptors Inhibition (32%) 1 mM HEK‐293 cells [49]
Nicotinic acetylcholine receptors No effect 10 Neonatal rat hypoglossal motor neurons [27]
Nicotinic acetylcholine receptors No effect 1–100 Cultured bovine adrenal chromaffin cells [81]
Glutamate transporters
[H3]‐glutamate uptake Potentiation (16%) 100 Rat cortical synaptosomes [101]
[H3]‐glutamate uptake Potentiation (27%) 100 GLAST glutamate transporter expressed in HEK‐293 cells [101]
[H3]‐glutamate uptake Potentiation (37%) 100 GLT1 glutamate transporter expressed in HEK‐293 cells [101]
[H3]‐glutamate uptake Potentiation (39%) 100 EAAC1 glutamate transporter expressed in HEK‐293 cells [101]
[H3]‐glutamate uptake Potentiation (67%) 0.1 Rat spinal cord synaptosomes [99]
(47%) 1
No effect >10
[H3]‐glutamate uptake Potentiation (25–30%) 10–300 Rat spinal cord synaptosomes [100]

aIC50.

bEC50.