ArticleeLife2023
Cannabidiol sensitizes TRPV2 channels to activation by 2-APB.
Article in eLife, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled it.
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Who cites it
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 29 citations in OpenAlex.
- Cannabidiol effects in stem cells: A systematic review.BioFactors (Oxford, England)Pooled it
- Structural origins of species-specific differences in TRPV2 activation.Nature communications · 2026Article
- Inactivation Switch for Run-up in TRPV2.Research square · 2026Article
- Transient receptor potential vanilloid 2 functions as a directional driver for hepoxilin AScience advances · 2026Article
- HaloTag-based approach to quantify subcellular localization of TRPV3 channels.Biophysical journal · 2026Article
- Cannabidiol exerts antiinflammatory effects but maintains T effector memory cell differentiation in humans.JCI insight · 2026Article
- TRPV2 and TRPC5 are potential targets for astringent phytochemicals.Current research in food science · 2026Article
- Cannabidiol does not cause DNA double-strand breaks in a human liver-derived cell model.Journal of cannabis research · 2025Article
- Carvone derived cannabidiol enantiomers as novel anticonvulsants.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Nongenomic Stimulatory Effect of T3 on Calcium Dynamics in GnRH Neurons via Integrin αVβ3.Endocrinology · 2025Article
- Pharmacokinetic analysis of selective TRPV2 inhibitor SET2 in rats.Scientific reports · 2025Article
- Molecular determinants of 2-aminoethoxydiphenyl borate sensitivity of transient receptor potential vanilloid 2-unexpected differences between 2 rodent orthologs.Molecular pharmacology · 2025Article
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Structure- and Ligand-Based Virtual Screening for Identification of Novel TRPV4 Antagonists.Molecules (Basel, Switzerland) · 2024Article
- Cannabinoid inhibition of mechanosensitive KbioRxiv : the preprint server for biology · 2024Article
- Experimental and computational biophysics to identify vasodilator drugs targeted at TRPV2 using agonists based on the probenecid scaffold.Computational and structural biotechnology journal · 2024Article
- TRPV2 calcium channel promotes breast cancer progression potential by activating autophagy.Cancer cell international · 2024Article
- Tyrosine phosphorylation and palmitoylation of TRPV2 ion channel tune microglial beta-amyloid peptide phagocytosis.Journal of neuroinflammation · 2024Article
- Unraveling the Mechanisms of Cannabidiol's Pharmacological Actions: A Comprehensive Research Overview.Topics in current chemistry (Cham) · 2024Review
- Functional and structural insights into activation of TRPV2 by weak acids.The EMBO journal · 2024Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The cation-permeable TRPV2 channel is important for cardiac and immune cell function. Cannabidiol (CBD), a non-psychoactive cannabinoid of clinical relevance, is one of the few molecules known to activate TRPV2. Using the patch-clamp technique, we discover that CBD can sensitize current responses of the rat TRPV2 channel to the synthetic agonist 2-aminoethoxydiphenyl borate (2-APB) by over two orders of magnitude, without sensitizing channels to activation by moderate (40°C) heat. Using cryo-EM, we uncover a new small-molecule binding site in the pore domain of rTRPV2 in addition to a nearby CBD site that had already been reported. The TRPV1 and TRPV3 channels are also activated by 2-APB and CBD and share multiple conserved features with TRPV2, but we find that strong sensitization by CBD is only observed in TRPV3, while sensitization for TRPV1 is much weaker. Mutations at non-conserved positions between rTRPV2 and rTRPV1 in either the pore domain or the CBD sites failed to confer strong sensitization by CBD in mutant rTRPV1 channels. Together, our results indicate that CBD-dependent sensitization of rTRPV2 channels engages multiple channel regions, and that the difference in sensitization strength between rTRPV2 and rTRPV1 channels does not originate from amino acid sequence differences at the CBD binding site or the pore domain. The remarkably robust effect of CBD on TRPV2 and TRPV3 channels offers a promising new tool to both understand and overcome one of the major roadblocks in the study of these channels - their resilience to activation.
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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.