Catalog Number: 2498
Chemical Name: N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea
Biological Activity
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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. 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
  3. 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;

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

8 Citations: Showing 1 - 8
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  1. Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors.
    Authors: daCosta Et al.
    J Neurosci 2015;6:8057
  2. Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus.
    Authors: John Et al.
    PLoS One 2015;1601:15
  3. 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
  4. Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.
    Authors: Zhang Et al.
    Mol Pharmacol 2015;10:e0137588
  5. 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
  6. Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons.
    Authors: Chatzidaki Et al.
    PLoS One 2015;10:e0125116
  7. 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
  8. 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

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