ArticleBritish journal of pharmacology2011
Stereo-selective inhibition of transient receptor potential TRPC5 cation channels by neuroactive steroids.
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 24 papers.
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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.
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Who cites it
24 citing papers in PubMed, 55 citations in OpenAlex.
- Therapeutic potential of transient receptor potential (TRP) channels in psychiatric disorders.Journal of neural transmission (Vienna, Austria : 1996) · 2024Review
- Review
- Altered Steroidome in Women with Gestational Diabetes Mellitus: Focus on Neuroactive and Immunomodulatory Steroids from the 24th Week of Pregnancy to Labor.Biomolecules · 2021Article
- The epithelial potassium channel Kir7.1 is stimulated by progesterone.The Journal of general physiology · 2021Article
- Review
- Aging, hormones and receptors.Physiological research · 2020Review
- Group 1 metabotropic glutamate receptors trigger glutamate-induced intracellular CaCellular and molecular life sciences : CMLS · 2020Article
- Antinociceptive Effects of Lipid Raft Disruptors, a Novel Carboxamido-Steroid and Methyl β-Cyclodextrin, in Mice by Inhibiting Transient Receptor Potential Vanilloid 1 and Ankyrin 1 Channel Activation.Frontiers in physiology · 2020Article
- Interfacial Binding Sites for Cholesterol on TRP Ion Channels.Biophysical journal · 2019Article
- Activation of Adrenal Steroidogenesis and an Improvement of Mood Balance in Postmenopausal Females after Spa Treatment Based on Physical Activity.International journal of molecular sciences · 2019Article
- Sex hormone intake in female blood donors: impact on haemolysis during cold storage and regulation of erythrocyte calcium influx by progesterone.Blood transfusion = Trasfusione del sangue · 2019Article
- Catechol estrogens stimulate insulin secretion in pancreatic β-cells via activation of the transient receptor potential A1 (TRPA1) channel.The Journal of biological chemistry · 2019Article
- Carboxamido steroids inhibit the opening properties of transient receptor potential ion channels by lipid raft modulation.Journal of lipid research · 2018Article
- TRPV2 is a novel biomarker and therapeutic target in triple negative breast cancer.Oncotarget · 2018Article
- Endothelial CaInternational journal of molecular sciences · 2018Review
- TRP Channels as Potential Targets for Sex-Related Differences in Migraine Pain.Frontiers in molecular biosciences · 2018Review
- Calcium-engaged Mechanisms of Nongenomic Action of Neurosteroids.Current neuropharmacology · 2017Review
- Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels.British journal of pharmacology · 2015Article
- Transient receptor potential (TRP) channels: a clinical perspective.British journal of pharmacology · 2014Review
- In pursuit of small molecule chemistry for calcium-permeable non-selective TRPC channels -- mirage or pot of gold?British journal of pharmacology · 2013Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 3 countries.
Funding
Abstract
background and purposeTransient receptor potential canonical 5 (TRPC5) channels are widely expressed, including in the CNS, where they potentiate fear responses. They also contribute to other non-selective cation channels that are stimulated by G-protein-coupled receptor agonists and lipid and redox factors. Steroids are known to modulate fear and anxiety states, and we therefore investigated whether TRPC5 exhibited sensitivity to steroids. EXPERIMENTAL APPROACH: Human TRPC5 channels were conditionally expressed in HEK293 cells and studied using intracellular Ca2+ measurement, whole-cell voltage-clamp and excised patch techniques. For comparison, control experiments were performed with cells lacking TRPC5 channels or expressing another TRP channel, TRPM2. Native TRPC channel activity was recorded from vascular smooth muscle cells. KEY
resultsExtracellular application of pregnenolone sulphate, pregnanolone sulphate, pregnanolone, progesterone or dihydrotestosterone inhibited TRPC5 activity within 1-2min. Dehydroepiandrosterone sulphate or 17β-oestradiol had weak inhibitory effects. Pregnenolone, and allopregnanolone, a progesterone metabolite and stereo-isomer of pregnanolone, all had no effects. Progesterone was the most potent of the steroids, especially against TRPC5 channel activity evoked by sphingosine-1-phosphate. In outside-out patch recordings, bath-applied progesterone and dihydrotestosterone had strong and reversible effects, suggesting relatively direct mechanisms of action. Progesterone inhibited native TRPC5-containing channel activity, evoked by oxidized phospholipid. CONCLUSIONS AND IMPLICATIONS: Our data suggest that TRPC5 channels are susceptible to relatively direct and rapid stereo-selective steroid modulation, leading to channel inhibition. The study adds to growing appreciation of TRP channels as non-genomic steroid sensors.
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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.