An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

@article{Shirey2008AnAP,
  title={An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.},
  author={Jana K. Shirey and Zixiu Xiang and Daniel J. Orton and Ashley E. Brady and Kari A. Johnson and Richard Franklin Williams and Jennifer Edl Ayala and Alice Lambert Rodriguez and J{\"u}rgen Wess and David E. Weaver and Colleen M Niswender and Peter Jeffrey Conn},
  journal={Nature chemical biology},
  year={2008},
  volume={4 1},
  pages={
          42-50
        }
}
Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of multiple central nervous system disorders. We have used cheminformatics and medicinal chemistry to develop new, highly selective M4 allosteric potentiators. VU10010, the lead compound, potentiates the M4 response to acetylcholine 47-fold while having no activity at other mAChR subtypes. This compound binds to an allosteric site on the receptor and increases affinity for acetylcholine and coupling to G… CONTINUE READING
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