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Allosteric modulators of the α4β2 subtype of neuronal nicotinic acetylcholine receptors
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DOI：10.1016/j.bcp.2011.04.020.png)
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Abstract
En 中文
Nicotinic acetylcholine receptors are ligand-gated ion conducting transmembrane channels from the Cys-loop receptor super-family. The alpha 4 beta 2 subtype is the predominant heteromeric subtype of nicotinic receptors found in the brain. Allosteric modulators for alpha 4 beta 2 receptors interact at a site other than the orthosteric site where acetylcholine binds. Many compounds which act as allosteric modulators of the alpha 4 beta 2 receptors have been identified, with both positive and negative effects. Such allosteric modulators either increase or decrease the response induced by agonist on the alpha 4 beta 2 receptors. Here we discuss the concept of allosterism as it pertains to the alpha 4 beta 2 receptors and summarize the important features of allosteric modulators for this nicotinic receptor subtype. Published by Elsevier Inc.
Keywords:
Nicotinic acetylcholine receptor
Allosteric modulation
Positive allosteric modulators
Negative allosteric modulators
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