The DOI matches its Crossref record; 35 of the 35 references it cites were found in a registry or an index.
Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation
Open accessAbstract
Despite the increasing interest in TRPA1 channel as a pain target, its role in cold sensation and body temperature regulation is not clear; the efficacy and particularly side effects resulting from channel blockade remain poorly understood. Here we use a potent, selective, and bioavailable antagonist to address these issues. A-967079 potently blocks human (IC(50): 51 nmol/L, electrophysiology, 67 nmol/L, Ca(2+) assay) and rat TRPA1 (IC(50): 101 nmol/L, electrophysiology, 289 nmol/L, Ca(2+) assay). It is >1000-fold selective over other TRP channels, and is >150-fold selective over 75 other ion channels, enzymes, and G-protein-coupled receptors. Oral dosing of A-967079 produces robust drug exposure in rodents, and exhibits analgesic efficacy in allyl isothiocyanate-induced nocifensive response and osteoarthritic pain in rats (ED(50): 23.2 mg/kg, p.o.). A-967079 attenuates cold allodynia produced by nerve injury but does not alter noxious cold sensation in naive animals, suggesting distinct roles of TRPA1 in physiological and pathological states. Unlike TRPV1 antagonists, A-967079 does not alter body temperature. It also does not produce locomotor or cardiovascular side effects. Collectively, these data provide novel insights into TRPA1 function and suggest that the selective TRPA1 blockade may present a viable strategy for alleviating pain without untoward side effects.
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Citations
Cites
ANKTM1, a TRP-like Channel Expressed in Nociceptive Neurons, Is Activated by Cold Temperatures
Story, G. M., Peier, A. M., Reeve, A. J., Eid, S. R., Mosbacher, J., Hricik, T. R., Earley, T. J., Hergarden, A. C., Andersson, D. A., Hwang, S. W., et al. (2003) · Cell · doi:10.1016/s0092-8674(03)00158-2 · Cited by 2,486
TRPA1 Mediates the Inflammatory Actions of Environmental Irritants and Proalgesic Agents
Bautista, D. M., Jordt, S.-E., Nikai, T., Tsuruda, P. R., Read, A. J., Poblete, J., Yamoah, E. N., Basbaum, A. I., & Julius, D. (2006) · Cell · doi:10.1016/j.cell.2006.02.023 · Cited by 1,932
Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1
Jordt, S.-E., Bautista, D. M., Chuang, H.-H., McKemy, D. D., Zygmunt, P. M., Högestätt, E. D., Meng, I. D., & Julius, D. (2004) · Nature · doi:10.1038/nature02282 · Cited by 1,899
Noxious Cold Ion Channel TRPA1 Is Activated by Pungent Compounds and Bradykinin
Bandell, M., Story, G. M., Hwang, S. W., Viswanath, V., Eid, S. R., Petrus, M. J., Earley, T. J., & Patapoutian, A. (2004) · Neuron · doi:10.1016/s0896-6273(04)00150-3 · Cited by 1,827
Kwan, K. Y., Allchorne, A. J., Vollrath, M. A., Christensen, A. P., Zhang, D.-S., Woolf, C. J., & Corey, D. P. (2006) · Neuron · doi:10.1016/j.neuron.2006.03.042 · Cited by 1,267
TRPA1 mediates formalin-induced pain
McNamara, C. R., Mandel-Brehm, J., Bautista, D. M., Siemens, J., Deranian, K. L., Zhao, M., Hayward, N. J., Chong, J. A., Julius, D., Moran, M. M., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0705924104 · Cited by 1,263
Trevisani, M., Siemens, J., Materazzi, S., Bautista, D. M., Nassini, R., Campi, B., Imamachi, N., Andrè, E., Patacchini, R., Cottrell, G. S., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0705923104 · Cited by 770
Obata, K. (2005) · Journal of Clinical Investigation · doi:10.1172/jci25437 · Cited by 630
TRPA1 acts as a cold sensor in vitro and in vivo
Karashima, Y., Talavera, K., Everaerts, W., Janssens, A., Kwan, K. Y., Vennekens, R., Nilius, B., & Voets, T. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0808487106 · Cited by 585
Jarvis, M. F., Honore, P., Shieh, C.-C., Chapman, M., Joshi, S., Zhang, X.-F., Kort, M., Carroll, W., Marron, B., Atkinson, R., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0611364104 · Cited by 528
Self-citation
Cited by
Skin temperature: its role in thermoregulation
Romanovsky, A. A. (2014) · Acta Physiologica · doi:10.1111/apha.12231 · Cited by 518
TRPA1 channels: molecular sentinels of cellular stress and tissue damage
Viana, F. (2016) · The Journal of Physiology · doi:10.1113/jp270935 · Cited by 210
The thermoregulation system and how it works
(2018) · Handbook of Clinical Neurology · doi:10.1016/b978-0-444-63912-7.00001-1 · Cited by 186
Transient Receptor Potential Channels in neuropathic pain
Basso, L., & Altier, C. (2017) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2016.10.002 · Cited by 134
TRPA1 mediates the hypothermic action of acetaminophen
Gentry, C., Andersson, D. A., & Bevan, S. (2015) · Scientific Reports · doi:10.1038/srep12771 · Cited by 50
Metadata
- Authors
- Chen, J., Joshi, S. K., DiDomenico, S., Perner, R. J., Mikusa, J. P., Gauvin, D. M., Segreti, J. A., Han, P., Zhang, X.-F., Niforatos, W., Bianchi, B. R., Baker, S. J., Zhong, C., Simler, G. H., McDonald, H. A., Schmidt, R. G., McGaraughty, S. P., Chu, K. L., Faltynek, C. R., Kort, M. E., Reilly, R. M., & Kym, P. R.
- Venue
- Pain
- Published
- 2011-05
- Volume
- 152
- Issue
- 5
- Pages
- 1165-1172
- ISSN
- 0304-3959 (ISSN-L)
- OpenAlex
- W1983037105
- Cited by
- 276
- References
- 35
- FWCI
- 11.16
- Type
- journal article
- Language
- en
- Open access
- green
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- Chen, J., Joshi, S. K., DiDomenico, S., Perner, R. J., Mikusa, J. P., Gauvin, D. M., Segreti, J. A., Han, P., Zhang, X.-F., Niforatos, W., Bianchi, B. R., Baker, S. J., Zhong, C., Simler, G. H., McDonald, H. A., Schmidt, R. G., McGaraughty, S. P., Chu, K. L., Faltynek, C. R., . . . Kym, P. R. (2011). Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation. Pain. https://doi.org/10.1016/j.pain.2011.01.049
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
