ArticleBritish journal of pharmacology2011
Rosiglitazone inhibits Kv4.3 potassium channels by open-channel block and acceleration of closed-state inactivation.
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.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 26 citations in OpenAlex.
- Acute arsenic trioxide inhibits the cardiac transient outward KCurrent research in structural biology · 2026Article
- Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2023Article
- Schizophrenia: a disorder of broken brain bioenergetics.Molecular psychiatry · 2022Review
- The antidiabetic drug rosiglitazone blocks Kv1.5 potassium channels in an open state.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2022Article
- Calcium/calmodulin-dependent protein kinase II associates with the KFrontiers in neuroanatomy · 2022Article
- Advances in PPARs Molecular Dynamics and Glitazones as a Repurposing Therapeutic Strategy through Mitochondrial Redox Dynamics against Neurodegeneration.Current neuropharmacology · 2022Review
- Computational Identification of Novel Kir6 Channel Inhibitors.Frontiers in pharmacology · 2019Article
- Raloxifene inhibits cloned Kv4.3 channels in an estrogen receptor-independent manner.Pflugers Archiv : European journal of physiology · 2015Article
- Minireview: Challenges and opportunities in development of PPAR agonists.Molecular endocrinology (Baltimore, Md.) · 2014Review
- Electromechanical and atrial and ventricular antiarrhythmic actions of CIJ-3-2F, a novel benzyl-furoquinoline vasodilator in rat heart.British journal of pharmacology · 2014Article
- Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Inhibition of Kv4.3 potassium channels by trazodone.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Auxiliary KChIP4a suppresses A-type K+ current through endoplasmic reticulum (ER) retention and promoting closed-state inactivation of Kv4 channels.The Journal of biological chemistry · 2013Article
- Properties and molecular determinants of the natural flavone acacetin for blocking hKv4.3 channels.PloS one · 2013Article
- Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.Journal of medicinal chemistry · 2012Article
- Article
- Cardiac ion channel modulation by the hypoglycaemic agent rosiglitazone.British journal of pharmacology · 2011Article
- Can the electrophysiological action of rosiglitazone explain its cardiac side effects?Current medicinal chemistry · 2011Article
Corrections and comments
- Commented on by
Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeRosiglitazone is a widely used oral hypoglycaemic agent, which improves insulin resistance in type 2 diabetes. Chronic rosiglitazone treatment is associated with a number of adverse cardiac events. The present study was designed to characterize the effects of rosiglitazone on cloned K(v)4.3 potassium channels. EXPERIMENTAL APPROACH: The interaction of rosiglitazone with cloned K(v)4.3 channels stably expressed in Chinese hamster ovary cells was investigated using whole-cell patch-clamp techniques. KEY
resultsRosiglitazone decreased the currents carried by K(v)4.3 channels and accelerated the current inactivation, concentration-dependently, with an IC(50) of 24.5 µM. The association and dissociation rate constants for rosiglitazone were 1.22 µM(-1)·s(-1) and 31.30 s(-1) respectively. Block by rosiglitazone was voltage-dependent, increasing in the voltage range for channel activation; however, no voltage dependence was found in the voltage range required for full activation. Rosiglitazone had no effect on either the deactivation kinetics or the steady-state activation of K(v)4.3 channels. Rosiglitazone shifted the steady-state inactivation curves in the hyperpolarizing direction, concentration-dependently. The K(i) for the interaction between rosiglitazone and the inactivated state of K(v)4.3 channels was 1.49 µM, from the concentration-dependent shift in the steady-state inactivation curves. Rosiglitazone also accelerated the kinetics of the closed-state inactivation of K(v)4.3 channels. Rosiglitazone did not affect either use dependence or recovery from inactivation of K(v)4.3 currents. CONCLUSION AND IMPLICATIONS: Our results indicate that rosiglitazone potently inhibits currents carried by K(v)4.3 channels by interacting with these channels in the open state and by accelerating the closed-state inactivation of K(v)4.3 channels.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.