N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA

The Uses of N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA

PNU 120596 is a type II positive allosteric modulator.

What are the applications of Application

PNU 120596 is a type II positive allosteric modulator

Definition

ChEBI: 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-3-isoxazolyl)urea is a member of ureas.

Biological Activity

Positive allosteric modulator of α 7 neuronal nicotinic acetylcholine receptors (EC 50 = 216 nM), with no detectable effect on α 4 β 2, α 3 β 4 and α 9 α 10 receptors. Active in vivo following systemic administration.

Biochem/physiol Actions

An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector.

Storage

Desiccate at +4°C

References

[1] hurst r s, hajós m, raggenbass m, et al. a novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. the journal of neuroscience, 2005, 25(17): 4396-4405.
[2] bertrand d, gopalakrishnan m. allosteric modulation of nicotinic acetylcholine receptors. biochemical pharmacology, 2007, 74(8): 1155-1163.