PNU-120,596

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PNU-120,596
(IUPAC) ime
1-(5-hloro-2,4-dimetoksifenil)-3-(5-metilizoksazol-3-il)ureja
Klinički podaci
Identifikatori
CAS broj 501925-31-1
ATC kod nije dodeljen
PubChem[1][2] 311434
ChEMBL[3] CHEMBL257591
Hemijski podaci
Formula C13H14ClN3O4 
Mol. masa 311,720
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

PNU-120,596 je lek koji deluje kao potentan i selektivan pozitivni alosterni modulator za α7 podtip neuronskih nikotinskih acetilholinskih receptora.[4][5] On se koristi u naučnim istraživanjima za izučavanje holinergične regulacije oslobađanja dopamina i glutamata u mozgu.[6][7][8]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. Hurst, R.; Hajós, M.; Raggenbass, M.; Wall, T.; Higdon, N.; Lawson, J.; Rutherford-Root, K.; Berkenpas, M.; Hoffmann, W. (2005). "A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization". Journal of Neuroscience 25 (17): 4396–4405. PMID 15858066. doi:10.1523/JNEUROSCI.5269-04.2005. 
  5. Young, G.; Zwart, R.; Walker, A.; Sher, E.; Millar, N. (2008). "Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site". Proceedings of the National Academy of Sciences of the United States of America 105 (38): 14686–14691. Bibcode:2008PNAS..10514686Y. PMC 2535569. PMID 18791069. doi:10.1073/pnas.0804372105. 
  6. Livingstone, P.; Srinivasan, J.; Kew, J.; Dawson, L.; Gotti, C.; Moretti, M.; Shoaib, M.; Wonnacott, S. (2009). "Alpha7 and non-alpha7 nicotinic acetylcholine receptors modulate dopamine release in vitro and in vivo in the rat prefrontal cortex". The European Journal of Neuroscience 29 (3): 539–550. PMID 19187266. doi:10.1111/j.1460-9568.2009.06613.x. 
  7. Barron, S.; Mclaughlin, J.; See, J.; Richards, V.; Rosenberg, R. (2009). "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". Molecular Pharmacology 76 (2): 253–263. PMC 2713121. PMID 19411608. doi:10.1124/mol.109.056226. 
  8. Livingstone, P.; Dickinson, J.; Srinivasan, J.; Kew, J.; Wonnacott, S. (2009). "Glutamate-Dopamine Crosstalk in the Rat Prefrontal Cortex is Modulated by Alpha7 Nicotinic Receptors and Potentiated by PNU-120596". Journal of molecular neuroscience : MN 40 (1-2): 172–176. PMID 19688191. doi:10.1007/s12031-009-9232-5. 

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