title: Transient receptor potential ankyrin 1 (TRPA1) antagonists.
abstract: The transient receptor potential ankyrin 1 (TRPA1) channel is an irritant sensor highly expressed on nociceptive neurons. The clinical use of TRPA1 antagonists is based on the concept that TRPA1 is active during disease states like neuropathic pain. Indeed, in Phase 2a proof-of-concept studies the TRPA1 antagonist GRC17536 has shown efficacy in patients with painful diabetic neuropathy. Moreover, animal studies suggest that the therapeutic value of TRPA1 antagonists extends beyond pain to pruritus, asthma and cough with limited safety concerns. This review provides a comprehensive overview of the patent literature (since 2007) on small-molecule inhibitors of the TRPA1 channel. Despite the clear progress, many unanswered questions remain. Future advancement to Phase 3 studies will assess the real translational potential of this research field.
authors: Department of Chemical & Pharmaceutical Sciences, University of Ferrara, Italy.
authors: Delia
authors: D
authors: Preti
authors: Giulia
authors: G
authors: Saponaro
authors: Arpad
authors: A
authors: Szallasi
mesh_terms: D000818:Animals; D015220:Calcium Channels; D055808:Drug Discovery; D004345:Drug Industry; D006801:Humans; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D010330:Patents as Topic; D000074025:TRPA1 Cation Channel; D050051:Transient Receptor Potential Channels / Q000037:antagonists & inhibitors*
chemical_list: D015220:Calcium Channels; D009419:Nerve Tissue Proteins; D000074025:TRPA1 Cation Channel; C473350:TRPA1 protein, human; D050051:Transient Receptor Potential Channels