ArticleJournal of molecular neuroscience : MN2013
Identification of molecular determinants for a potent mammalian TRPA1 antagonist by utilizing species differences.
Article in Journal of molecular neuroscience : MN, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 36 citations in OpenAlex.
- TRPA1 for Butterfly Eyespot Formation.International journal of molecular sciences · 2026Article
- Evolutionary adaptations of TRPA1 thermosensitivity and skin thermoregulation in vertebrates.iScience · 2025Article
- Insights into Molecular Interactions and Biological Effect of Natural Stilbenoids at the TRPA1 Ion Channel.ChemMedChem · 2025Article
- Discovery ofJournal of medicinal chemistry · 2023Article
- Differential sensitivity of cinnamaldehyde-evoked calcium fluxes to ruthenium red in guinea pig and mouse trigeminal sensory neurons.BMC research notes · 2021Article
- TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Non-Analgesic Symptomatic or Disease-Modifying Potential of TRPA1.Medical sciences (Basel, Switzerland) · 2019Review
- Computational Drug Repurposing Algorithm Targeting TRPA1 Calcium Channel as a Potential Therapeutic Solution for Multiple Sclerosis.Pharmaceutics · 2019Article
- Identification of possible hypoxia sensor for behavioral responses in a marine annelid,Biology open · 2019Article
- TRPA1 ankyrin repeat six interacts with a small molecule inhibitor chemotype.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Discovery of a Series of Indazole TRPA1 Antagonists.ACS medicinal chemistry letters · 2017Article
- Identification of a putative binding site critical for general anesthetic activation of TRPA1.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Evolutionary tuning of TRPA1 and TRPV1 thermal and chemical sensitivity in vertebrates.Temperature (Austin, Tex.) · 2017Review
- Structural basis of TRPA1 inhibition by HC-030031 utilizing species-specific differences.Scientific reports · 2016Article
- How the TRPA1 receptor transmits painful stimuli: Inner workings revealed by electron cryomicroscopy.BioEssays : news and reviews in molecular, cellular and developmental biology · 2015Review
- Article
- Deciphering Subtype-Selective Modulations in TRPA1 Biosensor Channels.Current neuropharmacology · 2015Review
- Molecular basis determining inhibition/activation of nociceptive receptor TRPA1 protein: a single amino acid dictates species-specific actions of the most potent mammalian TRPA1 antagonist.The Journal of biological chemistry · 2014Article
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The transient receptor potential A1 (TRPA1) receptor is a member of the TRP family and an excitatory nonselective cation channel. An increasing body of evidence suggests that TRPA1 acts as a nociceptor for various chemicals and physical stimuli. Thus, many TRPA1 antagonists have been developed as analgesic agents. Recently, we found that AP18, a mammalian TRPA1 antagonist, does not inhibit heterologously expressed western clawed frog TRPA1 (fTRPA1). Here, we show that fTRPA1 is also insensitive to A967079, one of the most potent mammalian TRPA1 antagonists. Neither heterologously nor endogenously expressed fTRPA1 was inhibited by A967079 upon activation by TRPA1 agonists. Mutant channel analyses revealed that two specific amino acid residues located within the putative fifth transmembrane domain were involved in the inhibitory action of A967079. Our findings and previous reports based on species differences in the sensitivity to TRPA1 antagonists provide novel insights into the structure-function relationship of TRPA1 and supply useful information in the search for new analgesic medicines targeting TRPA1.
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