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

J Med Chem. 2009 Feb 12;52(3):818-25. doi: 10.1021/jm800962k.


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.

MeSH terms

  • Biphenyl Compounds / chemical synthesis
  • Biphenyl Compounds / pharmacology
  • Calcium / metabolism
  • Combinatorial Chemistry Techniques
  • Drug Design
  • Humans
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology
  • Pyridazines / chemical synthesis*
  • Pyridazines / pharmacology
  • Receptors, G-Protein-Coupled / agonists*
  • Receptors, G-Protein-Coupled / physiology
  • Structure-Activity Relationship


  • Biphenyl Compounds
  • Piperazines
  • Pyridazines
  • Receptors, G-Protein-Coupled
  • mas-related gene-X1 receptor, human
  • Calcium