Lipoic-Based TRPA1/TRPV1 Antagonist to Treat Orofacial Pain
(2015) ACS Chemical Neuroscience — Vol. 6, n° 3, p. 380-385 (2015)
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- Abstract
- Inflammation of the trigeminal nerve is considered one of the most painful conditions known to humankind. The diagnosis is often difficult; moreover, safe and effective pharmacological treatments are lacking. A new molecule, ADM_12, formed by a lipoic and omotaurine residues covalently linked, is here reported. In vitro and in vivo tests showed that ADM_12 is a very attractive original compound presenting: i) a remarkable safe profile; ii) a high binding constant vs. TRPA1; iii) an intriguing behaviour vs. TRPV1 and iv) the ability to significantly and persistently reduce mechanical facial allodynia in rats. Noteworthy, testing ADM_12 we shed light on the unprecedented involvement of TRPA1 and TRPV1 channels in orofacial pain.
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Gualdani, R., Ceruti, S., Magni, G., Merli, D., Di Cesare Mannelli, L., Francesconi, O., Richichi, B., la Marca, G., Ghelardini, C., Moncelli, M. R., & Nativi, C. (2015). Lipoic-Based TRPA1/TRPV1 Antagonist to Treat Orofacial Pain. ACS Chemical Neuroscience, 6(3), 380-385. https://doi.org/10.1021/cn500248u (Original work published 2015)