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Beschreibung

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the alpha7 subtype of neural nicotinic acetylcholine receptors (EC50 = 216 nM), with no significant effect on alpha4beta2, alpha3beta4 and alpha9alpha10 receptors. Specifically increase a-7 nAChR-mediated channel currents and channel mean open time in cultured neurons (~ 1 mM). However, it does neither affect ion selectivity nor unitary conductance. Shown to cross the blood-brain barrier. Causes conformational changes in the ligand binding domain of a7 nicotinic receptors that partially overlap with those caused by acetylcholine. Causes changes in cysteine accessibility at the inner beta sheet, transition zone, and agonist binding site. Also reported to potentiate agonist-evoked GABAergic postsynaptic inward currents in somatodendritic membrane of hippocampal interneurons.