PNU-120,596 je lek koji deluje kao potentan i selektivan pozitivni alosterni modulator za α7 podtip neuronskih nikotinskih acetilholinskih receptora.[1][2] On se koristi u naučnim istraživanjima za izučavanje holinergične regulacije oslobađanja dopamina i glutamata u mozgu.[3][4][5]

PNU-120,596
IUPAC ime
1-(5-hloro-2,4-dimetoksifenil)-3-(5-metilizoksazol-3-il)ureja
Identifikatori
CAS broj501925-31-1 ДаY
ATC kodNone
PubChemCID 311434
ChEMBLCHEMBL257591
Hemijski podaci
FormulaC13H14ClN3O4
Molarna masa311,720
  • COc1cc(OC)c(Cl)cc1NC(=O)Nc2noc(C)c2

Reference уреди

  1. ^ 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.  |first10= захтева |last10= у Authors list (помоћ)
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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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