ArticleBritish journal of pharmacology2019
Potent, selective, and subunit-dependent activation of TRPC5 channels by a xanthine derivative.
Article in British journal of pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 46 citations in OpenAlex.
- (-)-Englerin A binding to human TRPC5 exposes an aromatic interaction network in channel activation.Nature communications · 2026Article
- Ideal efficacy photoswitching for chromocontrol of TRPC4/5 channel functions in live tissues.Nature chemical biology · 2026Article
- Molecular architecture of the human TRPC1/C5 heteromeric channel.Nature communications · 2025Article
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- Article
- TRPC5 controls the adrenaline-mediated counter regulation of hypoglycemia.The EMBO journal · 2024Article
- BTDAzo: A Photoswitchable TRPC5 Channel Activator.Angewandte Chemie (International ed. in English) · 2022Article
- Schwarzinicine A inhibits transient receptor potential canonical channels and exhibits overt vasorelaxation effects.Phytotherapy research : PTR · 2022Article
- TRPC5 is essential in endothelium-dependent contraction of aorta from diet-induced obese mice.Fundamental research · 2022Article
- DogCatcher allows loop-friendly protein-protein ligation.Cell chemical biology · 2022Article
- Nonselective TRPC channel inhibition and suppression of aminoglycoside-induced premature termination codon readthrough by the small molecule AC1903.The Journal of biological chemistry · 2022Article
- 29th Annual GP2A Medicinal Chemistry Conference.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Canonical transient receptor potential channels and their modulators: biology, pharmacology and therapeutic potentials.Archives of pharmacal research · 2021Review
- Article
- Xanthine-based photoaffinity probes allow assessment of ligand engagement by TRPC5 channels.RSC chemical biology · 2020Article
- Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site.Communications biology · 2020Article
- TRPC channels: Structure, function, regulation and recent advances in small molecular probes.Pharmacology & therapeutics · 2020Review
- Angiotensin-II-Evoked CaCells · 2020Article
- Canonical Transient Receptor Potential (TRPC) Channels in Nociception and Pathological Pain.Neural plasticity · 2020Review
- Transient Receptor Potential Cation Channels in Cancer Therapy.Medical sciences (Basel, Switzerland) · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeThe TRPC1, TRPC4, and TRPC5 proteins form homotetrameric or heterotetrameric, calcium-permeable cation channels that are involved in various disease states. Recent research has yielded specific and potent xanthine-based TRPC1/4/5 inhibitors. Here, we investigated the possibility of xanthine-based activators of these channels. EXPERIMENTAL APPROACH: An analogue of the TRPC1/4/5 inhibitor Pico145, AM237, was synthesized and its activity was investigated using HEK cells overexpressing TRPC4, TRPC5, TRPC4-C1, TRPC5-C1, TRPC1:C4 or TRPC1:C5 channels, and in A498 cells expressing native TRPC1:C4 channels. TRPC1/4/5 channel activities were assayed by measuring intracellular concentration of Ca KEY
resultsAM237 potently activated TRPC5:C5 channels (EC CONCLUSIONS AND IMPLICATIONS: This study suggests the possibility for selective activation of TRPC5 channels by xanthine derivatives and supports the general principle that xanthine-based compounds can activate, potentiate, or inhibit these channels depending on subunit composition.
Indexed as
Identifiers
What OpenQuestion holds
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.