Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors

  title={Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors},
  author={Jan Jakub{\'i}k and Alena Rand{\'a}kov{\'a} and Pavel Zim{\vc}{\'i}k and Esam E. El-Fakahany and Vladim{\'i}r Dole{\vz}al},
  journal={Scientific Reports},
Interaction of orthosteric ligands with extracellular domain was described at several aminergic G protein-coupled receptors, including muscarinic acetylcholine receptors. The orthosteric antagonists quinuclidinyl benzilate (QNB) and N-methylscopolamine (NMS) bind to the binding pocket of the muscarinic acetylcholine receptor formed by transmembrane α-helices. We show that high concentrations of either QNB or NMS slow down dissociation of their radiolabeled species from all five subtypes of… Expand
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