PNU-120596-CAS 501925-31-1-Calbiochem

C₁₃H₁₄ClN₃O₄

311.72

MFCD00095313

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.

Toxicity: Standard Handling (A)

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

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

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

100

≥99% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 100 mg/mL, clear, colorless

ambient

2-8℃

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3