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PNU-120596
α7 Neuronal Nicotinic Acetylcholine Receptor Agonist, PNU-120596, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea, a7 nAChR agonist, PNU-120596
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.
产品信息
Form White solid
Molar mass 311.7
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥99% by HPLC
Solubility DMSO
Chemical formula C13H14ClN3O4
CAS number 501925-31-1
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |