ArticleCell calcium2012
Pregnenolone sulphate-independent inhibition of TRPM3 channels by progesterone.
Article in Cell calcium, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers, 1 of them a synthesis that pooled it.
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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
31 citing papers in PubMed, 1 synthesis or guideline pooled it, 79 citations in OpenAlex.
- Mechanosensitive receptors in migraine: a systematic review.The journal of headache and pain · 2024Pooled it
- A duo of redox-sensitive pore-loop cysteines controls the activity of the neural ion channel TRPM3.Communications chemistry · 2026Article
- Sex difference in TRPM3 channel functioning in nociceptive and vascular systems: an emerging target for migraine therapy in females?The journal of headache and pain · 2025Review
- Functional Analysis of TRPA1, TRPM3, and TRPV1 Channels in Human Dermal Arteries and Their Role in Vascular Modulation.Pharmaceuticals (Basel, Switzerland) · 2024Article
- TRPM8 contributes to sex dimorphism by promoting recovery of normal sensitivity in a mouse model of chronic migraine.Nature communications · 2022Article
- Migraine-relevant sex-dependent activation of mouse meningeal afferents by TRPM3 agonists.The journal of headache and pain · 2022Article
- Steroid Sulfation in Neurodegenerative Diseases.Frontiers in molecular biosciences · 2022Review
- Steroids, steroid associated substances and gestational diabetes mellitus.Physiological research · 2021Review
- Partial Agonistic Actions of Sex Hormone Steroids on TRPM3 Function.International journal of molecular sciences · 2021Article
- 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
- TRPM3 in Brain (Patho)Physiology.Frontiers in cell and developmental biology · 2021Review
- TRPM Channels in Human Diseases.Cells · 2020Review
- The structural basis for an on-off switch controlling Gβγ-mediated inhibition of TRPM3 channels.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Steroids and TRP Channels: A Close Relationship.International journal of molecular sciences · 2020Review
- TRPM3_miR-204: a complex locus for eye development and disease.Human genomics · 2020Review
- Molecular and Mechanical Mechanisms Regulating Ductus Arteriosus Closure in Preterm Infants.Frontiers in pediatrics · 2020Review
- TRPM8-androgen receptor association within lipid rafts promotes prostate cancer cell migration.Cell death & disease · 2019Article
- Understanding the pathobiology in patent ductus arteriosus in prematurity-beyond prostaglandins and oxygen.Pediatric research · 2019Review
- Identification and classification of a new TRPM3 variant (γ subtype).The journal of physiological sciences : JPS · 2019Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 2 countries.
Funding
Abstract
Transient Receptor Potential Melastatin 3 (TRPM3) is a widely expressed calcium-permeable non-selective cation channel that is stimulated by high concentrations of nifedipine or by physiological steroids that include pregnenolone sulphate. Here we sought to identify steroids that inhibit TRPM3. Channel activity was studied using calcium-measurement and patch-clamp techniques. Progesterone (0.01-10μM) suppressed TRPM3 activity evoked by pregnenolone sulphate. Progesterone metabolites and 17β-oestradiol were also inhibitory but the effects were relatively small. Dihydrotestosterone was an inhibitor at concentrations higher than 1μM. Corticosteroids lacked effect. Overlay assays indicated that pregnenolone sulphate, progesterone and dihydrotestosterone bound to TRPM3. In contrast to dihydrotestosterone, progesterone inhibited nifedipine-evoked TRPM3 activity or activity in the absence of an exogenous activator, suggesting a pregnenolone sulphate-independent mechanism of action. Dihydrotestosterone, like a non-steroid look-alike compound, acted as a competitive antagonist at the pregnenolone sulphate binding site. Progesterone inhibited endogenous TRPM3 in vascular smooth muscle cells. Relevance of TRPM3 or the progesterone effect to ovarian cells, which have been suggested to express TRPM3, was not identified. The data further define a chemical framework for competition with pregnenolone sulphate at TRPM3 and expand knowledge of steroid interactions with TRPM3, suggesting direct steroid binding and pregnenolone sulphate-independent inhibition by progesterone.
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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.