Adamantyl analogues of paracetamol as potent analgesic drugs via inhibition of TRPA1
| Autor: | Susana Quirce, Ruth Pérez-Fernández, Antonio Ferrer-Montiel, Roberto de la Torre-Martínez, Pilar Goya, Carlos Goicoechea, M. Isabel Martín, Nieves Fresno, José Elguero, Asia Fernández-Carvajal, Ibon Alkorta |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Computer and Information Sciences Cannabinoid receptor Analgesic TRPV1 Pain lcsh:Medicine Pharmacology Pathology and Laboratory Medicine Chemical synthesis Cell Line Ab Initio Quantum Chemistry Methods Mice Signs and Symptoms Computational Chemistry Transient Receptor Potential Channels Medicine and Health Sciences Pain Management Animals Humans Medicine Antipyretic lcsh:Science Computerized Simulations Acetaminophen Analgesics Multidisciplinary business.industry Organic Chemistry lcsh:R digestive oral and skin physiology Antagonist Visceral Pain Chemistry Disease Models Animal Drug Design Physical Sciences lcsh:Q Medicinal Chemistry business Drug metabolism Research Article medicine.drug |
| Zdroj: | PLoS ONE, Vol 9, Iss 12, p e113841 (2014) PLoS ONE Digital.CSIC. Repositorio Institucional del CSIC instname |
| Popis: | Paracetamol also known as acetaminophen, is a widely used analgesic and antipyretic agent. We report the synthesis and biological evaluation of adamantyl analogues of paracetamol with important analgesic properties. The mechanism of nociception of compound 6a/b, an analog of paracetamol, is not exerted through direct interaction with cannabinoid receptors, nor by inhibiting COX. It behaves as an interesting selective TRPA1 channel antagonist, which may be responsible for its analgesic properties, whereas it has no effect on the TRPM8 nor TRPV1 channels. The possibility of replacing a phenyl ring by an adamantyl ring opens new avenues in other fields of medicinal chemistry. |
| Databáze: | OpenAIRE |
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