Open-Channel Blockers at the Human α4β2 Neuronal Nicotinic Acetylcholine Receptor

  title={Open-Channel Blockers at the Human $\alpha$4$\beta$2 Neuronal Nicotinic Acetylcholine Receptor},
  author={Bruno Buisson and Daniel Bertrand},
  journal={Molecular Pharmacology},
To extend our knowledge of the pharmacological profile of human α4β2 neuronal nicotinic receptors, we investigated the action of hexamethonium on the major brain human nicotinic acetylcholine receptor (nAChR) stably expressed in human embryonic kidney 293 cells. This compound displays all of the characteristics of an open-channel blocker at the human α4β2 nAChR: a voltage-dependent inhibition (more pronounced at hyperpolarized potentials), absence of competition, and use dependence. Moreover… 

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    Proceedings of the National Academy of Sciences of the United States of America
  • 1988
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