PNU-120,596
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]
IUPAC ime | |
---|---|
1-(5-hloro-2,4-dimetoksifenil)-3-(5-metilizoksazol-3-il)ureja | |
Identifikatori | |
CAS broj | 501925-31-1 |
ATC kod | None |
PubChem | CID 311434 |
ChEMBL | CHEMBL257591 |
Hemijski podaci | |
Formula | C13H14ClN3O4 |
Molarna masa | 311,720 |
|
Reference уреди
- ^ 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.
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у Authors list (помоћ) - ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.