Table 5.
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.