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 safety profile; (ii) a high binding constant versus TRPA1; (iii) an intriguing behavior versus TRPV1; and (iv) the ability to significantly and persistently reduce mechanical facial allodynia in rats. Noteworthy, by testing ADM_12, we shed light on the unprecedented involvement of TRPA1 and TRPV1 channels in orofacial pain.
Lipoic-Based TRPA1/TRPV1 antagonist to treat orofacial pain / R. Gualdani, S. Ceruti, G. Magni, D. Merli, L. Di Cesare Mannelli, O. Francesconi, B. Richichi, G. la Marca, C. Ghelardini, M.R. Moncelli, C. Nativi. - In: ACS CHEMICAL NEUROSCIENCE. - ISSN 1948-7193. - 6:3(2015 Mar 18), pp. 380-385.
|Titolo:||Lipoic-Based TRPA1/TRPV1 antagonist to treat orofacial pain|
CERUTI, STEFANIA MARIA (Secondo)
|Parole Chiave:||antiallodynic agents; Lipoic acid; trigeminal pain; TRP channels|
|Settore Scientifico Disciplinare:||Settore BIO/14 - Farmacologia|
Settore CHIM/06 - Chimica Organica
|Data di pubblicazione:||18-mar-2015|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1021/cn500248u|
|Appare nelle tipologie:||01 - Articolo su periodico|