- Guide to PHARMACOLOGY
Synonyms: AWD-21360 | D-23129 | ezogabine | Potiga® | Trobalt® | WAY-143841
retigabine is an approved drug (FDA and EMA (2011))
Compound class: Synthetic organic
Comment: Retigabine is unique among antiepileptic drugs in that it functions by activating selected voltage-gated potassium channels in the brain (i.e. Kv7 family channels)  .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: retigabine
1. Dupuis DS, Schrøder RL, Jespersen T, Christensen JK, Christophersen P, Jensen BS, Olesen SP. (2002)
Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.
Eur J Pharmacol, 437 (3): 129-37. [PMID:11890900]
2. Liu R, Tzounopoulos T, Wipf P. (2019)
Synthesis and Optimization of Kv7 (KCNQ) Potassium Channel Agonists: The Role of Fluorines in Potency and Selectivity.
ACS Med Chem Lett, 10 (6): 929-935. DOI: 10.1021/acsmedchemlett.9b00097 [PMID:31223450]
3. Main MJ, Cryan JE, Dupere JR, Cox B, Clare JJ, Burbidge SA. (2000)
Modulation of KCNQ2/3 potassium channels by the novel anticonvulsant retigabine.
Mol Pharmacol, 58 (2): 253-62. [PMID:10908292]
4. Rogawski MA, Bazil CW. (2008)
New molecular targets for antiepileptic drugs: alpha(2)delta, SV2A, and K(v)7/KCNQ/M potassium channels.
Curr Neurol Neurosci Rep, 8 (4): 345-52. [PMID:18590620]
5. Tatulian L, Delmas P, Abogadie FC, Brown DA. (2001)
Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine.
J Neurosci, 21 (15): 5535-45. [PMID:11466425]
6. Wainger BJ, Macklin EA, Vucic S, McIlduff CE, Paganoni S, Maragakis NJ, Bedlack R, Goyal NA, Rutkove SB, Lange DJ et al.. (2021)
Effect of Ezogabine on Cortical and Spinal Motor Neuron Excitability in Amyotrophic Lateral Sclerosis: A Randomized Clinical Trial.
JAMA Neurol, 78 (2): 186-196. [PMID:33226425]