Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.

@article{Bridges2009DiscoveryOT,
  title={Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.},
  author={Thomas M. Bridges and Joy Marlo and Colleen M Niswender and Carrie K Jones and Satyawan B Jadhav and Patrick R. Gentry and Hyekyung C Plumley and C David Weaver and P Jeffrey Conn and Craig W Lindsley},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 11},
  pages={3445-8}
}
This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays… CONTINUE READING