Article
Novel selective, potent naphthyl TRPM8 antagonists identified through a combined ligand- and structure-based virtual screening approach.
Scientific reports - 8 Sept 2017
Beccari Andrea R, Gemei Marica, Lo Monte Matteo, Menegatti Nazareno, Fanton Marco, Pedretti Alessandro, Bovolenta Silvia, Nucci Cinzia, Molteni Angela, Rossignoli Andrea, Brandolini Laura, Taddei Alessandro, Za Lorena, Liberati Chiara, Vistoli Giulio
Abstract excerpt
Transient receptor potential melastatin 8 (TRPM8), a nonselective cation channel, is the predominant mammalian cold temperature thermosensor and it is activated by cold temperatures and cooling compounds, such as menthol and icilin. Because of its role in cold allodynia, cold hyperalgesia and painful syndromes TRPM8 antagonists are currently being pursued as potential therapeutic agents for the treatment of pain...
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