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
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 / A. Moriello, L. Luongo, F. Guida, M. Christodoulou, D. Perdicchia, S. Maione, D. Passarella, V. Marzo, L. Petrocellis. - In: CNS & NEUROLOGICAL DISORDERS. DRUG TARGETS. - ISSN 1871-5273. - 15:8(2016 Oct), pp. 987-994. [10.2174/1871527315666160413123621]
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
M. Christodoulou;D. Perdicchia;D. Passarella;
2016
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 desensitizationFile | Dimensione | Formato | |
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CNS & Neurological Disorders - Drug Targets, 2016, 15, 987-994 proofs.pdf
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