ArticleMolecular brain2008
Development of selective blockers for Ca²(+)-activated Cl channel using Xenopus laevis oocytes with an improved drug screening strategy.
Article in Molecular brain, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 16 citations in OpenAlex.
- Article
- Evidence for tetrodotoxin-resistant spontaneous myogenic contractions of mouse isolated stomach that are dependent on acetylcholine.British journal of pharmacology · 2022Article
- The CaActa pharmaceutica Sinica. B · 2021Review
- Tonic Calcium-Activated Chloride Current Sustained by ATP Release and Highly Desensitizing Human P2X1 Receptors.Neuroscience · 2020Article
- A Single Natural Variation Determines Cytosolic CaMolecules and cells · 2020Article
- An Exploration of Charge Compensating Ion Channels across the Phagocytic Vacuole of Neutrophils.Frontiers in pharmacology · 2017Article
- Characterization of Rat Meibomian Gland Ion and Fluid Transport.Investigative ophthalmology & visual science · 2016Article
- Role of anoctamin-1 and bestrophin-1 in spinal nerve ligation-induced neuropathic pain in rats.Molecular pain · 2015Article
- Characterization of the effects of Cl⁻ channel modulators on TMEM16A and bestrophin-1 Ca²⁺ activated Cl⁻ channels.Pflugers Archiv : European journal of physiology · 2015Article
- Ano1, a Ca2+-activated Cl- channel, coordinates contractility in mouse intestine by Ca2+ transient coordination between interstitial cells of Cajal.The Journal of physiology · 2014Article
- Mas-related G protein-coupled receptor D is coupled to endogenous calcium-activated chloride channel in Xenopus oocytes.Journal of physiology and biochemistry · 2014Article
- MONNA, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1.Molecular pharmacology · 2013Article
- Flufenamic acid as an ion channel modulator.Pharmacology & therapeutics · 2013Review
- Regional differences in rat conjunctival ion transport activities.American journal of physiology. Cell physiology · 2012Article
- Calcium-activated chloride channels in the corpus cavernosum: recent developments and future of a key cellular component of the erectile process.International journal of impotence researchReview
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundCa²(+)-activated Cl⁻ channels (CaCCs) participate in many important physiological processes. However, the lack of effective and selective blockers has hindered the study of these channels, mostly due to the lack of good assay system. Here, we have developed a reliable drug screening method for better blockers of CaCCs, using the endogeneous CaCCs in Xenopus laevis oocytes and two-electrode voltage-clamp (TEVC) technique.
resultsOocytes were prepared with a treatment of Ca²(+) ionophore, which was followed by a treatment of thapsigargin which depletes Ca²(+) stores to eliminate any contribution of Ca²(+) release. TEVC was performed with micropipette containing chelerythrine to prevent PKC dependent run-up or run-down. Under these conditions, Ca²(+)-activated Cl⁻ currents induced by bath application of Ca²(+) to oocytes showed stable peak amplitude when repetitively activated, allowing us to test several concentrations of a test compound from one oocyte. Inhibitory activities of commercially available blockers and synthesized anthranilic acid derivatives were tested using this method. As a result, newly synthesized N-(4-trifluoromethylphenyl)anthranilic acid with trifluoromethyl group (-CF₃) at para position on the benzene ring showed the lowest IC₅₀.
conclusionOur results provide an optimal drug screening strategy suitable for high throughput screening, and propose N-(4-trifluoromethylphenyl)anthranilic acid as an improved CaCC blocker.
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