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 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.
Keywords:
Lipoic acid; TRP channels; antiallodynic agents; trigeminal pain.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Anti-Inflammatory Agents / chemistry
-
Anti-Inflammatory Agents / therapeutic use*
-
CHO Cells
-
Calcium Channels / genetics
-
Cricetulus
-
Dose-Response Relationship, Drug
-
Facial Pain / chemically induced
-
Facial Pain / drug therapy*
-
Glial Fibrillary Acidic Protein
-
Humans
-
Isothiocyanates / pharmacology
-
Nerve Tissue Proteins / antagonists & inhibitors*
-
Nerve Tissue Proteins / genetics
-
Patch-Clamp Techniques
-
Rats
-
TRPA1 Cation Channel
-
TRPV Cation Channels / metabolism
-
Thioctic Acid / therapeutic use*
-
Transfection
-
Transient Receptor Potential Channels / antagonists & inhibitors*
-
Transient Receptor Potential Channels / genetics
Substances
-
Anti-Inflammatory Agents
-
Calcium Channels
-
Glial Fibrillary Acidic Protein
-
Isothiocyanates
-
Nerve Tissue Proteins
-
TRPA1 Cation Channel
-
TRPA1 protein, human
-
TRPV Cation Channels
-
Transient Receptor Potential Channels
-
Trpv4 protein, rat
-
2,3,4-tri-O-acetylarabinopyranosyl isothiocyanate
-
Thioctic Acid