The DOI matches its Crossref record; 37 of the 37 references it cites were found in a registry or an index.
Activation of Expressed KCNQ Potassium Currents and Native Neuronal M-Type Potassium Currents by the Anti-Convulsant Drug Retigabine
Open accessAbstract
Retigabine [D-23129; N-(2-amino-4-(4-fluorobenzylamino)-phenyl) carbamic acid ethyl ester] is a novel anticonvulsant compound that is now in clinical phase II development. It has previously been shown to enhance currents generated by KCNQ2/3 K(+) channels when expressed in Chinese hamster ovary (CHO) cells (Main et al., 2000; Wickenden et al., 2000). In the present study, we have compared the actions of retigabine on KCNQ2/3 currents with those on currents generated by other members of the KCNQ family (homomeric KCNQ1, KCNQ2, KCNQ3, and KCNQ4 channels) expressed in CHO cells and on the native M current in rat sympathetic neurons [thought to be generated by KCNQ2/3 channels (Wang et al., 1998)]. Retigabine produced a hyperpolarizing shift of the activation curves for KCNQ2/3, KCNQ2, KCNQ3, and KCNQ4 currents with differential potencies in the following order: KCNQ3 > KCNQ2/3 > KCNQ2 > KCNQ4, as measured either by the maximum hyperpolarizing shift in the activation curves or by the EC(50) values. In contrast, retigabine did not enhance cardiac KCNQ1 currents. Retigabine also produced a hyperpolarizing shift in the activation curve for native M channels in rat sympathetic neurons. The retigabine-induced current was inhibited by muscarinic receptor stimulation, with similar agonist potency but 25% reduced maximum effect. In unclamped neurons, retigabine produced a hyperpolarization and reduced the number of action potentials produced by depolarizing current injections, without change in action potential configuration.
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Cites
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KvLQT1 and IsK (minK) proteins associate to form the IKS cardiac potassium current
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KCNQ2 and KCNQ3 Potassium Channel Subunits: Molecular Correlates of the M-Channel
Wang, H. (1998) · Science · doi:10.1126/science.282.5395.1890 · Cited by 1,294
A novel potassium channel gene, KCNQ2, is mutated in an inherited epilepsy of newborns
Singh, N. A., Charlier, C., Stauffer, D., DuPont, B. R., Leach, R. J., Melis, R., Ronen, G. M., Bjerre, I., Quattlebaum, T., Murphy, J. V., et al. (1998) · Nature Genetics · doi:10.1038/ng0198-25 · Cited by 1,199
A Potassium Channel Mutation in Neonatal Human Epilepsy
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Self-citation
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The neurobiology of antiepileptic drugs
Rogawski, M. A., & Löscher, W. (2004) · Nature Reviews Neuroscience · doi:10.1038/nrn1430 · Cited by 1,239
Pathways modulating neural KCNQ/M (Kv7) potassium channels
Delmas, P., & Brown, D. A. (2005) · Nature Reviews Neuroscience · doi:10.1038/nrn1785 · Cited by 686
Self-citationBrown, D. A., & Passmore, G. M. (2009) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2009.00111.x · Cited by 676
Self-citationMechanisms of action of currently used antiseizure drugs
Sills, G. J., & Rogawski, M. A. (2020) · Neuropharmacology · doi:10.1016/j.neuropharm.2020.107966 · Cited by 489
Molecular and cellular mechanisms of pharmacoresistance in epilepsy
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Metadata
- Authors
- Tatulian, L., Delmas, P., Abogadie, F. C., & Brown, D. A.
- Venue
- The Journal of Neuroscience
- Publisher
- Society for Neuroscience
- Published
- 2001-08-01
- Volume
- 21
- Issue
- 15
- Pages
- 5535-5545
- ISSN
- 0270-6474 (ISSN-L)
- 1529-2401
- OpenAlex
- W2168858520
- Cited by
- 406
- References
- 37
- FWCI
- 4.67
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Tatulian, L., Delmas, P., Abogadie, F. C., & Brown, D. A. (2001). Activation of Expressed KCNQ Potassium Currents and Native Neuronal M-Type Potassium Currents by the Anti-Convulsant Drug Retigabine. The Journal of Neuroscience. https://doi.org/10.1523/jneurosci.21-15-05535.2001
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