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

著者 Benallegue N , Mazzaferro S , Alcaino C , Bermudez I
Br J Pharmacol.2013 Sep ; 170(2):304-16.
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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 desensitization.
PMID: 23742319 [PubMed - indexed for MEDLINE]
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