Referenced in: none

Automatically associated channels: TRP , TRPA , TRPA1

Title: Chalcone derivatives activate and desensitize the transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 TRPA1 ion channel: structure-activity relationships in vitro and anti-nociceptive and anti-inflammatory activity in vivo.

Authors: A S Moriello, L Luongo, F Guida, M S Christodoulou, D Perdicchia, S Maione, D Passarella, V Di Marzo, L De Petrocellis

Journal, date & volume: CNS Neurol Disord Drug Targets, 2016 Apr 13 , ,

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/27071783

Abstract
Eleven compounds belonging to the chalcone family were tested for their ability to activate and subsequently desensitize the rat transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 (TRPA1) in a heterologous expression system. Four of the tested compounds were more potent than the TRPA1 agonist mustard oil, and showed also a strong desensitizing effect. Some chalcone compounds were not pungent in the eye-wiping assay and quite remarkably inhibited in a long-lasting and dose-dependent manner the pain response in the formalin test. Chalcones can be considered as novel candidates for the development of antihyperalgesic preparations based on TRPA1 desensitization.