Molecular structure of PNU 120596, CAS Number: 501925-31-1
PNU 120596 (CAS 501925-31-1)
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Alternate Names:
NSC 216666; N-(5-Chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)urea
Application:
PNU 120596 is a type II positive allosteric modulator
CAS Number:
501925-31-1
Molecular Weight:
311.72
Molecular Formula:
C13H14ClN3O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PNU 120596 is a type II positive allosteric modulator of alpha7 neuronal nicotinic acetylcholine receptor (AChR) located on the somatodendritic membrane of hippocampal interneurons. This modulator increases the frequency of acetylcholine-evoked GABAergic postsynaptic currents in pyramidal neurons, which can be suppressed by TTX. In addition, studies show that PNU 120596 increases the average time the channel of AChR is open, but does not have any effect on the selectivity of ions flowing through the channel. Furthermore, PNU 120596 has little effect on alpha4beta2, alpha3beta4 and alpha9alpha10 receptors. Alternate studies indicate that PNU 120596 increases the effects of choline on native alpha7-containing AChRs activating these receptors, thus producing single ion channel openings which result in an influx of calcium ions, that can be inhibited with the addition of methyllycaconitine.
PNU 120596 (CAS 501925-31-1) References
- A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. | Hurst, RS., et al. 2005. J Neurosci. 25: 4396-405. PMID: 15858066
- Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. | Grønlien, JH., et al. 2007. Mol Pharmacol. 72: 715-24. PMID: 17565004
- 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. | Barron, SC., et al. 2009. Mol Pharmacol. 76: 253-63. PMID: 19411608
- Physiological concentrations of choline activate native alpha7-containing nicotinic acetylcholine receptors in the presence of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea]. | Gusev, AG. and Uteshev, VV. 2010. J Pharmacol Exp Ther. 332: 588-98. PMID: 19923442
- Activation of functional α7-containing nAChRs in hippocampal CA1 pyramidal neurons by physiological levels of choline in the presence of PNU-120596. | Kalappa, BI., et al. 2010. PLoS One. 5: e13964. PMID: 21103043
- Investigation of the molecular mechanism of the α7 nicotinic acetylcholine receptor positive allosteric modulator PNU-120596 provides evidence for two distinct desensitized states. | Williams, DK., et al. 2011. Mol Pharmacol. 80: 1013-32. PMID: 21885620
- PNU-120596, a positive allosteric modulator of α7 nicotinic acetylcholine receptors, reverses a sub-chronic phencyclidine-induced cognitive deficit in the attentional set-shifting task in female rats. | McLean, SL., et al. 2012. J Psychopharmacol. 26: 1265-70. PMID: 22182741
- Protective effect of PNU-120596, a selective alpha7 nicotinic acetylcholine receptor-positive allosteric modulator, on myocardial ischemia-reperfusion injury in rats. | Li, H., et al. 2012. J Cardiovasc Pharmacol. 59: 507-13. PMID: 22343370
- The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. | Munro, G., et al. 2012. Br J Pharmacol. 167: 421-35. PMID: 22536953
- Positive allosteric modulator of α7 nicotinic-acetylcholine receptors, PNU-120596 augments the effects of donepezil on learning and memory in aged rodents and non-human primates. | Callahan, PM., et al. 2013. Neuropharmacology. 67: 201-12. PMID: 23168113
- The dual effect of PNU-120596 on α7 nicotinic acetylcholine receptor channels. | Kalappa, BI. and Uteshev, VV. 2013. Eur J Pharmacol. 718: 226-34. PMID: 24036349
- Mode of action of the positive modulator PNU-120596 on α7 nicotinic acetylcholine receptors. | Szabo, AK., et al. 2014. Neuropharmacology. 81: 42-54. PMID: 24486377
- An Unaltered Orthosteric Site and a Network of Long-Range Allosteric Interactions for PNU-120596 in α7 Nicotinic Acetylcholine Receptors. | Marotta, CB., et al. 2015. Chem Biol. 22: 1063-73. PMID: 26211363
- Effects of alpha-7 nicotinic allosteric modulator PNU 120596 on depressive-like behavior after lipopolysaccharide administration in mice. | Alzarea, S. and Rahman, S. 2018. Prog Neuropsychopharmacol Biol Psychiatry. 86: 218-228. PMID: 29800595
- PNU-120596, a positive allosteric modulator of mammalian α7 nicotinic acetylcholine receptor, is a negative modulator of ligand-gated chloride-selective channels of the gastropod Lymnaea stagnalis. | Vulfius, CA., et al. 2020. J Neurochem. 155: 274-284. PMID: 32248535
- PNU-120596, a positive allosteric modulator of α7 nicotinic acetylcholine receptor, directly inhibits p38 MAPK. | Uwada, J., et al. 2020. Biochem Pharmacol. 182: 114297. PMID: 33132165
- The α7 nAChR allosteric modulator PNU-120596 amends neuroinflammatory and motor consequences of parkinsonism in rats: Role of JAK2/NF-κB/GSk3β/ TNF-α pathway. | Gowayed, MA., et al. 2022. Biomed Pharmacother. 148: 112776. PMID: 35272136
Inhibitor of:
AChRα3, AChRα5, ATXN2L, and C10orf6.Activator of:
α9-nAChR, AChRε, ARHGAP39, C6orf134, KCNE3, RIC-3, and SK1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PNU 120596, 1 mg | sc-203200 | 1 mg | $31.00 | |||
PNU 120596, 5 mg | sc-203200A | 5 mg | $82.00 |