PNU 120596

Catalog #: 2498
15 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
2498/5
2498/25

PNU 120596 | CAS No. 501925-31-1 | Nicotinic (a7) Receptor Modulators

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Description: Positive allosteric modulator of α7 nAChRs; active in vivo

Chemical Name: N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea

Purity: ≥99%

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Product Details

Citations (15)

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Biological Activity

PNU 120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC₅₀ = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.

Technical Data

M.Wt:

311.72

Formula:

C₁₃H₁₄ClN₃O₄

Solubility:

Soluble to 100 mM in DMSO

Purity:

≥99%

Storage:

Desiccate at +4°C

CAS No:

501925-31-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization.
Hurst et al.
J.Neurosci., 2005;25:4396
An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo.
Timmermann et al.
J.Pharmacol.Exp.Ther., 2007;323:294
A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia.
Kalappa et al.
Br.J.Pharmacol. [Epub ahead of print], 2013;

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for PNU 120596

The citations listed below are publications that use Tocris products. Selected citations for PNU 120596 include:

15 Citations: Showing 1 - 10

Structure and gating mechanism of the α7 nicotinic acetylcholine receptor.
Authors: Noviello Et al.
Cell 2021;184:2121
Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo.
Authors: Bali Et al.
Sci Rep 2019;9:9324
Isomerization of Asp7 in Beta-Amyloid Enhances Inhibition of the α7 Nicotinic Receptor and Promotes Neurotoxicity.
Authors: Barykin Et al.
Cells 2019;8
Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens.
Authors: Gimenz-Gomez Et al.
Neuropharmacology 2018;135:581
Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors.
Authors: daCosta Et al.
J Neurosci 2015;6:8057
Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus.
Authors: John Et al.
PLoS One 2015;1601:15
6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor.
Authors: Kasheverov Et al.
Mar Drugs 2015;13:1255
Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.
Authors: Zhang Et al.
Mol Pharmacol 2015;10:e0137588
α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties.
Authors: Thomsen Et al.
PLoS One 2015;10:e0130572
Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons.
Authors: Chatzidaki Et al.
PLoS One 2015;10:e0125116

A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages.
Authors: Maldifassi Et al.
PLoS One 2014;9:e108397

Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT?a receptor antagonist.
Authors: Pandya and Yakel
Neuropharmacology 2013;70:35

Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates.
Authors: Yamauchi Et al.
Nat Commun 2012;82:687

Pharmacological characterization of native α7 nicotinic ACh receptors and their contribution to depolarization-elicited exocytosis in human chromaffin cells.
Authors: P&eacuterez-Alvarez Et al.
Br J Pharmacol 2012;165:908

Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes.
Authors: David Et al.
Eur J Neurosci 2010;31:978

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