ArticleBritish journal of pharmacology2013
Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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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
28 citing papers in PubMed, 50 citations in OpenAlex.
- Article
- TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy.Brain : a journal of neurology · 2023Article
- Sigma-1 Receptor Ligands Chlorpromazine and Trifluoperazine Attenuate CaCell and tissue biology · 2022Article
- Article
- Sigma1 Receptor Inhibits TRPC1-Mediated CaCellular and molecular neurobiology · 2021Article
- Axonal generation of amyloid-β from palmitoylated APP in mitochondria-associated endoplasmic reticulum membranes.Cell reports · 2021Article
- Sigmar1's Molecular, Cellular, and Biological Functions in Regulating Cellular Pathophysiology.Frontiers in physiology · 2021Review
- Factors Behind the Higher COVID-19 Risk in Diabetes: A Critical Review.Frontiers in public health · 2021Review
- VEGFC negatively regulates the growth and aggressiveness of medulloblastoma cells.Communications biology · 2020Article
- Sigma-1 receptor activation-induced glycolytic ATP production and endothelial barrier enhancement.Microcirculation (New York, N.Y. : 1994) · 2020Article
- Endothelial CaThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2020Review
- Hypertension, Thrombosis, Kidney Failure, and Diabetes: Is COVID-19 an Endothelial Disease? A Comprehensive Evaluation of Clinical and Basic Evidence.Journal of clinical medicine · 2020Review
- Is the sigma-1 receptor a potential pharmacological target for cardiac pathologies? A systematic review.International journal of cardiology. Heart & vasculature · 2020Review
- Neuroleptic Chlorpromazine Modulates CaDoklady. Biochemistry and biophysics · 2020Article
- Tubeimoside I Antagonizes Yoda1-Evoked Piezo1 Channel Activation.Frontiers in pharmacology · 2020Article
- The Molecular Function of σ Receptors: Past, Present, and Future.Trends in pharmacological sciences · 2019Review
- Transient Receptor Potential Channels and Endothelial Cell Calcium Signaling.Comprehensive Physiology · 2019Review
- Sigma-1 Receptor Antagonist Haloperidol Attenuates Store-Dependent CaDoklady. Biochemistry and biophysics · 2018Article
- TRPV1 channels and the progesterone receptor Sig-1R interact to regulate pain.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Blockade of sigma 1 receptors alleviates sensory signs of diabetic neuropathy in rats.European journal of pain (London, England) · 2017Article
Corrections and comments
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Authors and funding
17 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeThe Sigma-1 receptor (Sig1R) impacts on calcium ion signalling and has a plethora of ligands. This study investigated Sig1R and its ligands in relation to endogenous calcium events of endothelial cells and transient receptor potential (TRP) channels. EXPERIMENTAL APPROACH: Intracellular calcium and patch clamp measurements were made from human saphenous vein endothelial cells and HEK 293 cells expressing exogenous human TRPC5, TRPM2 or TRPM3. Sig1R ligands were applied and short interfering RNA was used to deplete Sig1R. TRP channels tagged with fluorescent proteins were used for subcellular localization studies. KEY
resultsIn endothelial cells, 10-100 μM of the Sig1R antagonist BD1063 inhibited sustained but not transient calcium responses evoked by histamine. The Sig1R agonist 4-IBP and related antagonist BD1047 were also inhibitory. The Sig1R agonist SKF10047 had no effect. Sustained calcium entry evoked by VEGF or hydrogen peroxide was also inhibited by BD1063, BD1047 or 4-IBP, but not SKF10047. 4-IBP, BD1047 and BD1063 inhibited TRPC5 or TRPM3, but not TRPM2. Inhibitory effects of BD1047 were rapid in onset and readily reversed on washout. SKF10047 inhibited TRPC5 but not TRPM3 or TRPM2. Depletion of Sig1R did not prevent the inhibitory actions of BD1063 or BD1047 and Sig1R did not co-localize with TRPC5 or TRPM3. CONCLUSIONS AND IMPLICATIONS: The data suggest that two types of Sig1R ligand (BD1047/BD1063 and 4-IBP) are inhibitors of receptor- or chemically activated calcium entry channels, acting relatively directly and independently of the Sig1R. Chemical foundations for TRP channel inhibitors are suggested.
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