ArticleBritish journal of pharmacology2015
TRPM4 inhibitor 9-phenanthrol activates endothelial cell intermediate conductance calcium-activated potassium channels in rat isolated mesenteric artery.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 42 citations in OpenAlex.
- The TRP channels serving as chemical-to-electrical signal converter.Physiological reviews · 2025Review
- Transient Receptor Potential Channels in Vascular Mechanotransduction.American journal of hypertension · 2025Review
- Role of transient receptor potential channels in the regulation of vascular tone.Drug discovery today · 2024Review
- Vascular mechanotransduction.Physiological reviews · 2023Review
- A Central Role for TRPM4 in CaInternational journal of molecular sciences · 2022Article
- Pharmacological Modulation and (Patho)Physiological Roles of TRPM4 Channel-Part 1: Modulation of TRPM4.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Article
- Transient receptor potential channels in sensory mechanisms of the lower urinary tract.Nature reviews. Urology · 2021Review
- TRPM4 in Cancer-A New Potential Drug Target.Biomolecules · 2021Review
- Actions of FTY720 (Fingolimod), a Sphingosine-1-Phosphate Receptor Modulator, on Delayed-Rectifier KMolecules (Basel, Switzerland) · 2020Article
- Morphological and pharmacological characterization of the porcine popliteal artery: A novel model for study of lower limb arterial disease.Microcirculation (New York, N.Y. : 1994) · 2019Article
- Functional Interaction among KInternational journal of molecular sciences · 2019Review
- High Effectiveness in Actions of Carfilzomib on Delayed-Rectifier KFrontiers in pharmacology · 2019Article
- The transient receptor potential melastatin 4 channel inhibitor 9-phenanthrol modulates cardiac sodium channel.British journal of pharmacology · 2018Article
- Involvement of TRPM4 in detrusor overactivity following spinal cord transection in mice.Naunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.British journal of pharmacology · 2018Article
- Identification of Resveratrol, an Herbal Compound, as an Activator of the Calcium-Activated Chloride Channel, TMEM16A.The Journal of membrane biology · 2017Article
- 9-Phenanthrol modulates postinhibitory rebound and afterhyperpolarizing potentials in an excitatory motor neuron of the medicinal leech.Journal of comparative physiology. A, Neuroethology, sensory, neural, and behavioral physiology · 2017Article
- A TRPM4 Inhibitor 9-Phenanthrol Inhibits Glucose- and Glucagon-Like Peptide 1-Induced Insulin Secretion from Rat Islets of Langerhans.Journal of diabetes research · 2017Article
- Novel regulatory mechanism in human urinary bladder: central role of transient receptor potential melastatin 4 channels in detrusor smooth muscle function.American journal of physiology. Cell physiology · 2016Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
background and purposeSmooth muscle transient receptor potential melastatin 4 (TRPM4) channels play a fundamental role in the development of the myogenic arterial constriction that is necessary for blood flow autoregulation. As TRPM4 channels are present throughout the vasculature, we investigated their potential role in non-myogenic resistance arteries using the TRPM4 inhibitor 9-phenanthrol. EXPERIMENTAL APPROACH: Pressure and wire myography were used to assess the reactivity of rat arteries, the latter in combination with measurements of smooth muscle membrane potential. Immunohistochemistry (IHC) and endothelial cell (EC) calcium changes were assessed in pressurized vessels and patch clamp measurements made in isolated ECs. KEY
resultsThe TRPM4 inhibitor 9-phenanthrol reversibly hyperpolarized mesenteric arteries to circa EK and blocked α1 -adrenoceptor-mediated vasoconstriction. Hyperpolarization was abolished and vasoconstriction re-established by damaging the endothelium. In mesenteric and cerebral artery smooth muscle, 9-phenanthrol hyperpolarization was effectively blocked by the KCa 3.1 inhibitor TRAM-34. 9-Phenanthrol did not increase mesenteric EC [Ca(2+)]i , and Na(+) substitution with N-methyl-D-glucamine only increased the muscle resting potential by 10 mV. Immunolabelling for TRPM4 was restricted to the endothelium and perivascular tissue. CONCLUSIONS AND IMPLICATIONS: These data reveal a previously unrecognized action of the TRPM4 inhibitor 9-phenanthrol - the ability to act as an activator of EC KCa 3.1 channels. They do not indicate a functionally important role for TRPM4 channels in the reactivity of non-myogenic mesenteric arteries.
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