Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor

K Chojnacka, RL Papke, NA Horenstein

Index: Chojnacka, Kinga; Papke, Roger L.; Horenstein, Nicole A. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 14 p. 4145 - 4149

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Citation Number: 14

Abstract

We introduce the term 'silent agonists' to describe ligands that can place the α7 nicotinic acetylcholine receptor (nAChR) into a desensitized state with little or no apparent activation of the ion channel, forming a complex that can subsequently generate currents when treated with an allosteric modulator. KC-1 (5′-phenylanabaseine) was synthesized and identified as a new silent agonist for the α7 nAChR; it binds to the receptor but does not activate α7 ...

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