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

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

Journal Name: CNS & Neurological Disorders - Drug Targets

Volume 15 , Issue 8 , 2016

Become EABM
Become Reviewer

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.

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

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 15
ISSUE: 8
Year: 2016
Page: [987 - 994]
Pages: 8
DOI: 10.2174/1871527315666160413123621
Price: $58

Article Metrics

PDF: 25
HTML: 3
EPUB: 1
PRC: 1