Biochemical Pharmacology volume 78, issue 7, P844-851 2009 DOI: 10.1016/j.bcp.2009.06.024 View full text
David J. Anderson, John Malysz, Jens Halvard Grønlien, Rachid El Kouhen, Monika Håkerud, Caroline Wetterstrand, Clark A. Briggs, Murali Gopalakrishnan

Abstract: alpha4beta2 neuronal nicotinic receptors (nAChRs) can exist in high and low sensitivity states possibly due to distinct stoichiometries during subunit assembly: (alpha4)(2)(beta2)(3) pentamer (high sensitivity, HS) and (alpha4)(3)(beta2)(2) pentamer (low sensitivity, LS). To determine if there is a linkage between HS or LS states and receptor-mediated responses in brain, we profiled several clinically studied alpha4beta2* nAChR agonists for the displacement of radioligand binding to alpha4beta2 [(3)H]-cytisine…

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