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TRPA1 antagonists as potential analgesic drugs.
Pharmacol Ther. 2012 Feb; 133(2):189-204.P&T

Abstract

The necessity of safe and effective treatments for chronic pain has intensified the search for new analgesic drugs. In the last few years, members of a closely-related family of ion channels, called transient receptor potential (TRP) have been identified in different cell types and their functions in physiological and pathological conditions have been characterized. The transient receptor potential ankyrin 1 (TRPA1), originally called ANKTM1 (ankyrin-like with transmembrane domains protein 1), is a molecule that has been conserved in different species during evolution; TRPA1 is a cation channel that functions as a cellular sensor, detecting mechanical, chemical and thermal stimuli, being a component of neuronal, epithelial, blood and smooth muscle tissues. In mammals, TRPA1 is largely expressed in primary sensory neurons that mediate somatosensory processes and nociceptive transmission. Recent studies have described the role of TRPA1 in inflammatory and neuropathic pain. However, its participation in cold sensation has not been agreed in different studies. In this review, we focus on data that support the relevance of the activation and blockade of TRPA1 in pain transmission, as well as the mechanisms underlying its activation and modulation by exogenous and endogenous stimuli. We also discuss recent advances in the search for new analgesic medicines targeting the TRPA1 channel.

Authors+Show Affiliations

Departamento de Farmacologia, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

22119554

Citation

Andrade, E L., et al. "TRPA1 Antagonists as Potential Analgesic Drugs." Pharmacology & Therapeutics, vol. 133, no. 2, 2012, pp. 189-204.
Andrade EL, Meotti FC, Calixto JB. TRPA1 antagonists as potential analgesic drugs. Pharmacol Ther. 2012;133(2):189-204.
Andrade, E. L., Meotti, F. C., & Calixto, J. B. (2012). TRPA1 antagonists as potential analgesic drugs. Pharmacology & Therapeutics, 133(2), 189-204. https://doi.org/10.1016/j.pharmthera.2011.10.008
Andrade EL, Meotti FC, Calixto JB. TRPA1 Antagonists as Potential Analgesic Drugs. Pharmacol Ther. 2012;133(2):189-204. PubMed PMID: 22119554.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - TRPA1 antagonists as potential analgesic drugs. AU - Andrade,E L, AU - Meotti,F C, AU - Calixto,J B, Y1 - 2011/11/15/ PY - 2011/10/27/received PY - 2011/10/29/accepted PY - 2011/11/29/entrez PY - 2011/11/29/pubmed PY - 2012/5/24/medline SP - 189 EP - 204 JF - Pharmacology & therapeutics JO - Pharmacol Ther VL - 133 IS - 2 N2 - The necessity of safe and effective treatments for chronic pain has intensified the search for new analgesic drugs. In the last few years, members of a closely-related family of ion channels, called transient receptor potential (TRP) have been identified in different cell types and their functions in physiological and pathological conditions have been characterized. The transient receptor potential ankyrin 1 (TRPA1), originally called ANKTM1 (ankyrin-like with transmembrane domains protein 1), is a molecule that has been conserved in different species during evolution; TRPA1 is a cation channel that functions as a cellular sensor, detecting mechanical, chemical and thermal stimuli, being a component of neuronal, epithelial, blood and smooth muscle tissues. In mammals, TRPA1 is largely expressed in primary sensory neurons that mediate somatosensory processes and nociceptive transmission. Recent studies have described the role of TRPA1 in inflammatory and neuropathic pain. However, its participation in cold sensation has not been agreed in different studies. In this review, we focus on data that support the relevance of the activation and blockade of TRPA1 in pain transmission, as well as the mechanisms underlying its activation and modulation by exogenous and endogenous stimuli. We also discuss recent advances in the search for new analgesic medicines targeting the TRPA1 channel. SN - 1879-016X UR - https://www.unboundmedicine.com/medline/citation/22119554/TRPA1_antagonists_as_potential_analgesic_drugs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0163-7258(11)00204-X DB - PRIME DP - Unbound Medicine ER -