PubMed 25546551

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPA , TRPA1 , TRPV , TRPV1

Title: Lipoic-based TRPA1/TRPV1 antagonist to treat orofacial pain.

Authors: Roberta Gualdani, Stefania Ceruti, Giulia Magni, Davide Merli, Lorenzo Di Cesare Mannelli, Oscar Francesconi, Barbara Richichi, Giancarlo la Marca, Carla Ghelardini, Maria Rosa Moncelli, Cristina Nativi

Journal, date & volume: ACS Chem Neurosci, 2015 Mar 18 , 6, 380-5

PubMed link:

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.