PNU-120,596

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	311434
ChEMBL	CHEMBL257591
Hemijski podaci
Formula	C13H14ClN3O4
Mol. masa	311,720
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C13H14ClN3O4/c1-7-4-12(17-21-7)16-13(18)15-9-5-8(14)10(19-2)6-11(9)20-3/h4-6H,1-3H3,(H2,15,16,17,18) ; Key: CEIIEALEIHQDBX-UHFFFAOYSA-N
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

↑ 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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ 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.
↑ 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. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Hurst, R.; Hajós, M.; Raggenbass, M.; Wall, T.; Higdon, N.; Lawson, J.; Rutherford-Root, K.; Berkenpas, M. i dr.. (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. DOI:10.1523/JNEUROSCI.5269-04.2005. PMID 15858066.
↑ 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. DOI:10.1073/pnas.0804372105. PMC 2535569. PMID 18791069.
↑ 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. DOI:10.1111/j.1460-9568.2009.06613.x. PMID 19187266.
↑ 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. DOI:10.1124/mol.109.056226. PMC 2713121. PMID 19411608.
↑ 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. DOI:10.1007/s12031-009-9232-5. PMID 19688191.

Vanjske veze

	Portal Medicina
	Portal Hemija

[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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. 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. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[4] Hurst, R.; Hajós, M.; Raggenbass, M.; Wall, T.; Higdon, N.; Lawson, J.; Rutherford-Root, K.; Berkenpas, M. i dr.. (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. DOI:10.1523/JNEUROSCI.5269-04.2005. PMID 15858066.

[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. DOI:10.1073/pnas.0804372105. PMC 2535569. PMID 18791069.

[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. DOI:10.1111/j.1460-9568.2009.06613.x. PMID 19187266.

[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. DOI:10.1124/mol.109.056226. PMC 2713121. PMID 19411608.

[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. DOI:10.1007/s12031-009-9232-5. PMID 19688191.

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Reference

Vanjske veze

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