Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor.

@article{Jakubk2002AllostericMB,
  title={Allosteric modulation by persistent binding of xanomeline of the interaction of competitive ligands with the M1 muscarinic acetylcholine receptor.},
  author={Jan Jakub{\'i}k and Stanislav Tu{\vc}ek and Esam E. El-Fakahany},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={301 3},
  pages={1033-41}
}
Xanomeline is a potent agonist that is functionally selective for muscarinic M(1) receptors. We have shown previously that a significant fraction of xanomeline binding to membranes of Chinese hamster ovary (CHO) cells expressing the M(1) receptors occurs in a wash-resistant manner and speculated that this persistent binding likely does not take place at the primary binding site on the receptor. In the present work we investigated in depth the pharmacological characteristics of this unique mode… CONTINUE READING

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