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Cat. No. Name Size Price Add Cart
KI3445PNU-120596QuoteQuote

Chemical Characteristic

Product NamePNU-120596
CAS No.501925-31-1
Molecular Weight 311.72096
FormulaC13H14ClN3O4
Chemical Name1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-1,2-oxazol-3-yl)urea
SmilesN(C(=O)Nc1noc(c1)C)c1c(cc(c(c1)Cl)OC)OC
Chemical Structure

Biological activities

PNU-120596 is a positive allosteric modulator of α7 nAChR with an EC50 of 216 nM.[1] Meanwhile, the EC50s of PNU-120596 for N52C and W148C mutant receptors are 340 and 450 nM, respectively.[2] PNU-120596 is used to treat psychiatric and neurological disorders. PNU-120596 causes changes in cysteine accessibility at the inner beta sheet, transition zone and agonist binding site while binding to α7 nAChR.[3] In addition, PNU-120596 causes reductions in the rate of modification of M37C and M40C.[2] PNU-120596 increases agonist (Ach)-evoked calcium flux mediated by an engineered variant of the human α7 nAChR.[3] PNU-120596 induces conformational changes along alternative pathways that lower energetic barriers to activation and lead to positive modulation.[1] In vitro, PNU-120596 markedly enhances α7 nAChR function in rat hippocampal interneurons. Furthermore, PNU-120596 modulates GABAergic synaptic transmission in isolated brain slices.[3] In vivo, in animal models, PNU-120596 (i.v. 1 mg/kg) significantly reverses the amphetamine-induced gating deficit, a common symptom of schizophrenia.[2]

Protocols

In vivo, PNU-120596 is dissolved in 15% methyl- b-cyclodextrin(15% MBCD).[4]

References

[1]Young GT, et al. Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci U S A. 2008, 105(38):14686-14691.
[2]Barron SC, et al. An allosteric modulator of alpha7 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 acetylcholine. Mol Pharmacol. 2009, 76(2):253-263.
[3]Hurst RS, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci. 2005, 25(17):4396-4405.
[4]Munro G, et al. The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. Br J Pharmacol. 2012, 167(2):421-435.

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