The additional ACh binding site at the α4(+)/α4(-) interface of the (α4β2)2α4 nicotinic ACh receptor contributes to desensitization.

@article{Benallegue2013TheAA,
  title={The additional ACh binding site at the α4(+)/α4(-) interface of the (α4β2)2α4 nicotinic ACh receptor contributes to desensitization.},
  author={Na{\"i}l Benallegue and Simone Mazzaferro and Constanza Alcaino and Isabel Bermudez},
  journal={British journal of pharmacology},
  year={2013},
  volume={170 2},
  pages={304-16}
}
BACKGROUND AND PURPOSE Nicotinic ACh (α4β2)2α4 receptors are highly prone to desensitization by prolonged exposure to low concentrations of agonist. Here, we report on the sensitivity of the three agonist sites of the (α4β2)2α4 to desensitization induced by prolonged exposure to ACh. We present electrophysiological data that show that the agonist sites of the (α4β2)2α4 receptor have different sensitivity to desensitization and that full receptor occupation decreases sensitivity to… CONTINUE READING

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