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Morten S. Thomsen and Jens D. Mikkelsen Type I and II positive allosteric modulators differentially modulate agonist-induced up-regulation of α7 nicotinic acetylcholine receptors Journal of Neurochemistry 123

Version of Record online: 16 AUG 2012 | DOI: 10.1111/j.1471-4159.2012.07876.x

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It is difficult to distinguish between the actions of type I and II positive allosteric modulators (PAMs) in vivo. Here, we show that only type II PAMs inhibit agonist-induced up-regulation of α7 nicotinic receptors in vivo. As up-regulation may be an important physiological response to receptor activation, this exacts caution in the development of type II PAMs.

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