ArticleBritish journal of pharmacology2011
Characteristics and molecular basis of celecoxib modulation on K(v)7 potassium channels.
Article in British journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 40 citations in OpenAlex.
- Cannabidiol inhibits both human KActa pharmacologica Sinica · 2026Article
- Functions of the KCNE Gene Family in Ion Channels.Biochemical genetics · 2026Review
- Galangin, a novel Kv7 potassium channel opener, exerts potent antinociceptive effects in multiple chronic pain mouse models.Acta pharmacologica Sinica · 2026Article
- Chemical modulation of Kv7 potassium channels.RSC medicinal chemistry · 2021Review
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- Antinociceptive Activity of Petroleum Ether Fraction ofBioMed research international · 2019Article
- Celecoxib Ameliorates Seizure Susceptibility in Autosomal Dominant Lateral Temporal Epilepsy.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- COX-2-selective inhibitors celecoxib and deracoxib modulate transient receptor potential vanilloid 3 channels.British journal of pharmacology · 2017Article
- Influence of CYP2C9 and COX-2 Genetic Polymorphisms on Clinical Efficacy of Non-Steroidal Anti-Inflammatory Drugs in Treatment of Ankylosing Spondylitis.Medical science monitor : international medical journal of experimental and clinical research · 2017Article
- Selective activation of vascular KBritish journal of pharmacology · 2016Article
- Article
- Evidence of more ion channels inhibited by celecoxib: KV1.3 and L-type Ca(2+) channels.BMC research notes · 2015Article
- KCNQ (Kv7) potassium channel activators as bronchodilators: combination with a β2-adrenergic agonist enhances relaxation of rat airways.American journal of physiology. Lung cellular and molecular physiology · 2014Article
- Potassium channels in peripheral pain pathways: expression, function and therapeutic potential.Current neuropharmacology · 2013Article
- The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)-benzamid displays anticonvulsant potential.British journal of pharmacology · 2013Article
- Modulation of K(v)7 potassium channels by a novel opener pyrazolo[1,5-a]pyrimidin-7(4H)-one compound QO-58.British journal of pharmacology · 2013Article
- Article
- One man's side effect is another man's therapeutic opportunity: targeting Kv7 channels in smooth muscle disorders.British journal of pharmacology · 2013Review
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeCelecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used for the treatment of pain and inflammation. Emerging and accumulating evidence suggests that celecoxib can affect cellular targets other than COX, such as ion channels. In this study, we characterized the effects of celecoxib on K(v)7 K(+) channels and compared its effects with the well-established K(v)7 channel opener retigabine. EXPERIMENTAL APPROACH: A perforated whole-cell patch technique was used to record K(v)7currents expressed in HEK 293 cells and M-type currents from rat superior cervical ganglion neurons. KEY
resultsCelecoxib enhanced K(v)7.2-7.4, K(v)7.2/7.3 and K(v)7.3/7.5 currents but inhibited K(v)7.1 and K(v)7.1/KCNE1 currents and these effects were concentration dependent. The IC(50) value for inhibition of K(v)7.1 channels was approximately 4 µM and the EC(50) values for activation of K(v)7.2-7.4, K(v)7.2/K(v)7.3 and K(v)7.3/K(v)7.5 channels were approximately 2-5 µM. The effects of celecoxib were manifested by increasing current amplitudes, shifting the voltage-dependent activation curve in a more negative direction and slowing the deactivation of K(v)7 currents. 2,5-Dimethyl-celecoxib, a celecoxib analogue devoid of COX inhibition activity, has similar but greater effects on K(v)7currents. K(v)7.2(A235T) and K(v) 7.2(W236L) mutant channels, which have greatly attenuated responses to retigabine, showed a reversed response to celecoxib, from activation to inhibition. CONCLUSIONS AND IMPLICATIONS: These results suggest that K(v)7 channels are targets of celecoxib action and provide new mechanistic evidence for understanding the effects of celecoxib. They also provide a new approach to developing K(v)7 modulators and for studying the structure-function relationship of K(v)7 channels.
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