General description

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors (EC₅₀ = 216 nM), 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hurst, R., et al. 2005. J. Neurosci. 25, 4396.Barron, S., et al. 2009. Mol. Pharm.76, 253.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)