2-3-4-tri-o-acetylarabinopyranosyl-isothiocyanate and Facial-Pain

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.

Topics: Animals; Anti-Inflammatory Agents; Calcium Channels; CHO Cells; Cricetulus; Dose-Response Relationship, Drug; Facial Pain; Glial Fibrillary Acidic Protein; Humans; Isothiocyanates; Nerve Tissue Proteins; Patch-Clamp Techniques; Rats; Thioctic Acid; Transfection; Transient Receptor Potential Channels; TRPA1 Cation Channel; TRPV Cation Channels