ArticleJournal of cellular physiology2012
Niflumic acid blocks native and recombinant T-type channels.
Article in Journal of cellular physiology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers, 1 of them a synthesis that pooled it.
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Who cites it
18 citing papers in PubMed, 1 synthesis or guideline pooled it, 38 citations in OpenAlex.
- Calcium channelopathies and intellectual disability: a systematic review.Orphanet journal of rare diseases · 2021Pooled it
- Chloride Intracellular Channel 4 (CLIC4) controls volume regulation in sperm development via Protein Kinase C (PKC).BMC biology · 2026Article
- Duality of Simplicity and Accuracy in QSPR: A Machine Learning Framework for Predicting Solubility of Selected Pharmaceutical Acids in Deep Eutectic Solvents.Molecules (Basel, Switzerland) · 2025Article
- Nonsteroidal Anti-Inflammatory Drugs as Modulators of Cation Channels: Fenamates Repurposing in Channelopathies.ChemMedChem · 2025Review
- ANO1 channels are expressed in mouse urethral smooth muscle but do not contribute to agonist or neurally evoked contractions.Scientific reports · 2025Article
- Mapping the rat gastric slow-wave conduction pathway: bridging in vitro and in vivo methods, revealing a loosely coupled region in the distal stomach.American journal of physiology. Gastrointestinal and liver physiology · 2024Article
- The rat acute oral toxicity of trifluoromethyl compounds (TFMs): a computational toxicology study combining the 2D-QSTR, read-across and consensus modeling methods.Archives of toxicology · 2024Article
- An in vivo drug screen in zebrafish reveals that cyclooxygenase 2-derived prostaglandin DCell proliferation · 2024Article
- Chaperone activity of niflumic acid on ClC-1 chloride channel mutants causing myotonia congenita.Frontiers in pharmacology · 2022Article
- Emerging Roles for Ion Channels in Ovarian Cancer: Pathomechanisms and Pharmacological Treatment.Cancers · 2021Review
- Normal Calcium-Activated Anion Secretion in a Mouse Selectively Lacking TMEM16A in Intestinal Epithelium.Frontiers in physiology · 2019Article
- Developmental Changes in the Inhibition of Glycinergic Synaptic Currents by Niflumic Acid in Hypoglossal Motoneurons.Frontiers in molecular neuroscience · 2018Article
- Possible roles for ATP release from RBCs exclude the cAMP-mediated Panx1 pathway.American journal of physiology. Cell physiology · 2017Article
- Niflumic acid, a TRPV1 channel modulator, ameliorates stavudine-induced neuropathic pain.Inflammopharmacology · 2016Article
- Flow cytometry analysis reveals that only a subpopulation of mouse sperm undergoes hyperpolarization during capacitation.Biology of reproduction · 2015Article
- T-type Ca2+ channels in spermatogenic cells and sperm.Pflugers Archiv : European journal of physiology · 2014Review
- Low concentrations of niflumic acid enhance basal spontaneous and carbachol-induced contractions of the detrusor.International urology and nephrology · 2014Article
- Anoctamin-1 in the juvenile rat urinary bladder.PloS one · 2014Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Voltage-dependent calcium channels are widely distributed in animal cells, including spermatozoa. Calcium is fundamental in many sperm functions such as: motility, capacitation, and the acrosome reaction (AR), all essential for fertilization. Pharmacological evidence has suggested T-type calcium channels participate in the AR. Niflumic acid (NA), a non-steroidal anti-inflammatory drug commonly used as chloride channel blocker, blocks T-currents in mouse spermatogenic cells and Cl(-) channels in testicular sperm. Here we examine the mechanism of NA blockade and explore if it can be used to separate the contribution of different Ca(V)3 members previously detected in these cells. Electrophysiological patch-clamp recordings were performed in isolated mouse spermatogenic cells and in HEK cells heterologously expressing Ca(V)3 channels. NA blocks mouse spermatogenic cell T-type currents with an IC(50) of 73.5 µM, without major voltage-dependent effects. The NA blockade is more potent in the open and in the inactivated state than in the closed state of the T-type channels. Interestingly, we found that heterologously expressed Ca(V)3.1 and Ca(V)3.3 channels were more sensitive to NA than Ca(V)3.2 channels, and this drug substantially slowed the recovery from inactivation of the three isoforms. Molecular docking modeling of drug-channel binding predicts that NA binds preferentially to the extracellular face of Ca(V)3.1 channels. The biophysical characteristics of mouse spermatogenic cell T-type currents more closely resemble those from heterologously expressed Ca(V)3.1 channels, including their sensitivity to NA. As Ca(V)3.1 null mice maintain their spermatogenic cell T-currents, it is likely that a novel Ca(V)3.2 isoform is responsible for them.
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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.