Multiple modes of α7 nAChR noncompetitive antagonism of control agonist-evoked and allosterically enhanced currents.

@article{Peng2013MultipleMO,
  title={Multiple modes of α7 nAChR noncompetitive antagonism of control agonist-evoked and allosterically enhanced currents.},
  author={Can Peng and Matthew R Kimbrell and Chengju Tian and Thomas F. Pack and Peter A. Crooks and Espero Kim Fifer and Roger L Papke},
  journal={Molecular pharmacology},
  year={2013},
  volume={84 3},
  pages={459-75}
}
Positive allosteric modulators (PAMs) of α7 nicotinic acetylcholine receptors can enhance ion channel currents and downstream effects of α7 stimulation. We investigated the approach of using noncompetitive antagonists to regulate α7 receptor function, potentially distinguishing effects requiring ion channel currents from signaling induced by nonconducting states. Three small readily reversible antagonists, (1S,2R,4R)-N,2,3,3-tetramethylbicyclo[2.2.1]heptan-2-amine (mecamylamine), N-(2.6… CONTINUE READING

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