Adamantyl analogues of paracetamol as potent analgesic drugs via inhibition of TRPA1
| العنوان: | Adamantyl analogues of paracetamol as potent analgesic drugs via inhibition of TRPA1 |
|---|---|
| المؤلفون: | 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 |
| المصدر: | PLoS ONE, Vol 9, Iss 12, p e113841 (2014) PLoS ONE Digital.CSIC. Repositorio Institucional del CSIC instname |
| بيانات النشر: | Public Library of Science, 2014. |
| سنة النشر: | 2014 |
| مصطلحات موضوعية: | 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 |
| الوصف: | 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. |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bc83bcde237a7e83a5989f3ca1833f9Test http://hdl.handle.net/10261/109392Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....1bc83bcde237a7e83a5989f3ca1833f9 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |