Description

• A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors (EC 50 = 216nM), with no significant effect on α4β2, α3β4 and α9α10 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.