ArticlePloS one2012
Inhibition of diacylglycerol-sensitive TRPC channels by synthetic and natural steroids.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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.
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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
19 citing papers in PubMed, 46 citations in OpenAlex.
- Pathophysiological significance and modulation of the transient receptor potential canonical 3 ion channel.Medicinal research reviews · 2024Review
- Review
- Increased transient receptor potential canonical 3 activity is involved in the pathogenesis of detrusor overactivity by dynamic interaction with NaLaboratory investigation; a journal of technical methods and pathology · 2022Article
- The epithelial potassium channel Kir7.1 is stimulated by progesterone.The Journal of general physiology · 2021Article
- Two transcriptionally distinct pathways drive female development in a reptile with both genetic and temperature dependent sex determination.PLoS genetics · 2021Article
- Activation of TRPV4 channels leads to a consistent tocolytic effect on human myometrial tissues.European journal of obstetrics & gynecology and reproductive biology: X · 2021Article
- TRPC channels: Structure, function, regulation and recent advances in small molecular probes.Pharmacology & therapeutics · 2020Review
- TRPM8-androgen receptor association within lipid rafts promotes prostate cancer cell migration.Cell death & disease · 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
- In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- TRP Channels as Potential Targets for Sex-Related Differences in Migraine Pain.Frontiers in molecular biosciences · 2018Review
- Pharmacological inhibition of focal segmental glomerulosclerosis-related, gain of function mutants of TRPC6 channels by semi-synthetic derivatives of larixol.British journal of pharmacology · 2017Article
- Ryanodine and IPNeurophotonics · 2017Article
- The Role of Transient Receptor Potential Channel 6 Channels in the Pulmonary Vasculature.Frontiers in immunology · 2017Review
- IL-17 induces MIP-1α expression in primary mouse astrocytes via TRPC channel.Inflammopharmacology · 2016Article
- Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels.British journal of pharmacology · 2015Article
- Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels.British journal of pharmacology · 2015Article
- Canonical transient receptor potential 4 and its small molecule modulators.Science China. Life sciences · 2015Review
- 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
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
TRPC channels are a family of nonselective cation channels that regulate ion homeostasis and intracellular Ca(2+) signaling in numerous cell types. Important physiological functions such as vasoregulation, neuronal growth, and pheromone recognition have been assigned to this class of ion channels. Despite their physiological relevance, few selective pharmacological tools are available to study TRPC channel function. We, therefore, screened a selection of pharmacologically active compounds for TRPC modulating activity. We found that the synthetic gestagen norgestimate inhibited diacylglycerol-sensitive TRPC3 and TRPC6 with IC(50)s of 3-5 µM, while half-maximal inhibition of TRPC5 required significantly higher compound concentrations (>10 µM). Norgestimate blocked TRPC-mediated vasopressin-induced cation currents in A7r5 smooth muscle cells and caused vasorelaxation of isolated rat aorta, indicating that norgestimate could be an interesting tool for the investigation of TRP channel function in native cells and tissues. The steroid hormone progesterone, which is structurally related to norgestimate, also inhibited TRPC channel activity with IC(50)s ranging from 6 to 18 µM but showed little subtype selectivity. Thus, TRPC channel inhibition by high gestational levels of progesterone may contribute to the physiological decrease of uterine contractility and immunosuppression during pregnancy.
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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.