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Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human

The P2X7 receptor is a calcium permeable cationic channel activated by extracellular ATP, playing a role in chronic pain, osteoporosis and arthritis. A number of potential lead compounds are inactive against the rat isoform, despite good activity against the human homologue, making animal model stud...

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Bibliographic Details
Published in:Bioorg Med Chem Lett
Main Authors: Caseley, Emily A., Muench, Stephen P., Baldwin, Stephen A., Simmons, Katie, Fishwick, Colin W., Jiang, Lin-Hua
Format: Artigo
Language:Inglês
Published: Elsevier Science Ltd 2015
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4508345/
https://ncbi.nlm.nih.gov/pubmed/26099538
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.06.001
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