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Biochem Pharmacol. 2013 Oct 15;86(8):1054-62. doi: 10.1016/j.bcp.2013.05.018. Epub 2013 May 31.

Effects of neuronal nicotinic acetylcholine receptor allosteric modulators in animal behavior studies.

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  • 1Chukchi Campus, Department of Bio-science, College of Rural and Community Development, University of Alaska Fairbanks, P.O. Box 297, Kotzebue, AK 99752-0297, USA. Electronic address:


Nicotinic acetylcholine receptors (nAChRs) are ligand-gated cation-conducting transmembrane channels from the cys-loop receptor superfamily. The neuronal subtypes of these receptors (e.g. the α7 and α4β2 subtypes) are involved in neurobehavioral processes such as anxiety, the central processing of pain, food intake, nicotine seeking behavior, and a number of cognitive functions like learning and memory. Neuronal nAChR dysfunction is involved in the pathophysiology of many neurological disorders, and behavioral studies in animals are useful models to assess the effects of compounds that act on these receptors. Allosteric modulators are ligands that bind to the receptors at sites other than the orthosteric site where acetylcholine, the endogenous agonist for the nAChRs, binds. While conventional ligands for the neuronal nAChRs have been studied for their behavioral effects in animals, allosteric modulators for these receptors have only recently gained attention, and research on their behavioral effects is growing rapidly. Here we will discuss the behavioral effects of allosteric modulators of the neuronal nAChRs.

Published by Elsevier Inc.


ACh; Allosteric modulation; NAM; PAM; acetylcholine; animal behavioral studies; cognition; nAChRs; negative allosteric modulator; neuronal nicotinic acetylcholine receptors; nicotinic acetylcholine receptor; pain; positive allosteric modulator; positive allosteric modulators

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