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

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

Volume: 15 Issue: 8

Author(s): Aniello Schiano Moriello, Livio Luongo, Francesca Guida, Michael S. Christodoulou, Dario Perdicchia, Sabatino Maione, Daniele Passarella, Vincenzo Di Marzo and Luciano De Petrocellis

Affiliation:

Keywords: Chalcones, eye wiping, neuropathic pain, pain, TRPA1.

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.

Cite this article as:

Moriello Schiano Aniello, Luongo Livio, Guida Francesca, Christodoulou S. Michael, Perdicchia Dario, Maione Sabatino, Passarella Daniele, Marzo Di Vincenzo and Petrocellis De Luciano, 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, CNS & Neurological Disorders - Drug Targets 2016; 15 (8) . https://dx.doi.org/10.2174/1871527315666160413123621