TRPA1 modulators in preclinical development

Expert Opinion on Therapeutic Patents
Felix Viana, Antonio Ferrer-Montiel

Abstract

Transient receptor potential ankyrin 1 (TRPA1) has been revealed as a pivotal molecular entity in sensory biology, especially as a sensor of chemical irritants present in foods, atmospheric pollutants and neurotoxic compounds. In addition, this channel appears responsible for detecting physical signals such as noxious cold and mechanical forces. There is mounting evidence that TRPA1 is involved in the pathophysiology of several diseases, and directly contributes to the cold and mechanical hyperalgesia present in inflammatory and neuropathic states. Therefore, TRPA1 is an important therapeutic target for drug development. Intriguingly, however, the number of receptor antagonists reported thus far is notably low, as compared with the large number of receptor agonists. Nonetheless, known TRPA1 antagonists display very promising in vivo activity against mechanical hypersensitivity and cold hyperalgesia, although at therapeutic doses that are still high for drug development. A significant effort is being pursued using medicinal chemistry programs to modify the initial scaffolds for evolving lead compounds for preclinical and clinical assays. It is anticipated that this field will blossom in the near future, and the number and therap...Continue Reading

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Citations

Oct 4, 2011·Lung·Megan S GraceMaria G Belvisi
Jan 19, 2011·ACS Chemical Neuroscience·Félix Viana
Aug 4, 2012·ACS Chemical Neuroscience·Sonali S Bharate, Sandip B Bharate
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Jul 30, 2011·British Journal of Pharmacology·Laura VayPeter A McNaughton
Apr 16, 2016·The Journal of Physiology·Félix Viana
Jan 1, 2011·Pharmaceuticals·Asia Fernández-CarvajalAntonio Ferrer-Montiel
Sep 1, 2010·Expert Review of Clinical Pharmacology·Laura VayPeter A McNaughton
Jun 5, 2014·The Journal of Pharmacology and Experimental Therapeutics·Ki Jeong LeeNarender R Gavva
Feb 11, 2011·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Pierluigi ValenteAntonio Ferrer-Montiel
Jul 21, 2020·Expert Opinion on Therapeutic Patents·Huifen Chen, Jack A Terrett
Jun 25, 2019·Frontiers in Pharmacology·Aurélien HaustrateV'yacheslav Lehen'kyi
Apr 2, 2010·Journal of Medicinal Chemistry·Pier Giovanni BaraldiPierangelo Geppetti

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