The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor

B Wroblowski, MJ Wigglesworth…

文献索引：Wroblowski, Berthold; Wigglesworth, Mark J.; Szekeres, Philip G.; Smith, Graham D.; Rahman, Shahzad S.; Nicholson, Neville H.; Muir, Alison I.; Hall, Adrian; Heer, Jag P.; Garland, Stephen L.; Coates, William J. Journal of Medicinal Chemistry, 2009 , vol. 52, # 3 p. 818 - 825

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被引用次数: 16

摘要

The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial docking studies of this ligand into the receptor in order to provide a suitable lead and tool compound for the elucidation of the physiological function of the receptor.