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CNS & Neurological Disorders - Drug Targets


ISSN (Print): 1871-5273
ISSN (Online): 1996-3181

Research Article

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 and Luciano De Petrocellis

Volume 15 , Issue 8 , 2016

Page: [987 - 994] Pages: 8

DOI: 10.2174/1871527315666160413123621

Price: $65


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.

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