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Ryckmans T Aubdool AA Bodkin JV Cox P Brain SD Dupont T Fairman E Hashizume Y Ishii N Kato T Kitching L Newman J Omoto K Rawson D Strover J 《Bioorganic & medicinal chemistry letters》2011,21(16):4857-4859
TrpA1 is an ion channel involved in nociceptive and inflammatory pain. It is implicated in the detection of chemical irritants through covalent binding to a cysteine-rich intracellular region of the protein. While performing an HTS of the Pfizer chemical collection, a class of pyrimidines emerged as a non-reactive, non-covalently binding family of agonists of the rat and human TrpA1 channel. Given the issues identified with the reference agonist Mustard Oil (MO) in screening, a new, non-covalently binding agonist was optimized and proved to be a superior agent to MO for screening purposes. Compound 16a (PF-4840154) is a potent, selective agonist of the rat and human TrpA1 channel and elicited TrpA1-mediated nocifensive behaviour in mouse. 相似文献
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Mohd-Taib Farah Shafawati Mohd-Saleh Wardah Asyikha Rosha Mansor Mohammad Saiful Ahmad-Mustapha Muzzneena Mustafa-Bakray Nur Aqilah Mod-Husin Shahril Md-Shukor Aisah Amat-Darbis Nurul Darsani Sulaiman Norela 《Wetlands Ecology and Management》2020,28(3):479-494
Wetlands Ecology and Management - Around the world, mangrove ecosystem has faced major threats from human activities, and birds were unexceptionally impacted. Mangrove fringe a large extent of the... 相似文献
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