SCH-58261

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SCH-58261
(IUPAC) ime
5-Amino-7-(2-feniletil)-2-(2-furil)-pirazolo(4,3-e)-1,2,4-triazolo(1,5-c)pirimidin
Klinički podaci
Identifikatori
CAS broj 160098-96-4
ATC kod nije dodeljen
PubChem[1][2] 176408
ChemSpider[3] 153647
ChEMBL[4] CHEMBL17127 DaY
Hemijski podaci
Formula C18H15N7O 
Mol. masa 345,357 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status nije kontrolisan

SCH-58261 je lek koji se koristi kao potentan i selektivan antagonist za adenozinski receptor A2A, sa više od 50x većim afinitetom za A2A u odnosu na druge adenozinske receptore.[5] On je korišten za istraživanje mehanizma dejstva kofeina, koji je mešoviti A1 / A2A antagonist, i pokazano je da je A2A receptor prvenstveno odgovoran za stimulantno dejstvo kofeina, dok je blokada oba, A1 i A2A, receptora potrebna za precizno reprodukovanje dejstva kofeina kod životinja.[6][7][8][9] Takođe je pokazano da SCH-58261 ima antidepresivno[10] i neuroprotektivno dejstvo u nizu modela na životinjama,[11][12][13][14][15] i on je istraživan kao mogući tretman za Parkinsonovu bolest.[16][17]

Reference[uredi | uredi kod]

  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. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ 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
  5. ↑ Zocchi C, Ongini E, Conti A, Monopoli A, Negretti A, Baraldi PG, Dionisotti S (February 1996). „The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist”. The Journal of Pharmacology and Experimental Therapeutics 276 (2): 398–404. PMID 8632302. 
  6. ↑ Svenningsson P, Nomikos GG, Ongini E, Fredholm BB (August 1997). „Antagonism of adenosine A2A receptors underlies the behavioural activating effect of caffeine and is associated with reduced expression of messenger RNA for NGFI-A and NGFI-B in caudate-putamen and nucleus accumbens”. Neuroscience 79 (3): 753–64. DOI:10.1016/S0306-4522(97)00046-8. PMID 9219939. 
  7. ↑ Popoli P, Reggio R, Pèzzola A, Fuxe K, Ferré S (July 1998). „Adenosine A1 and A2A receptor antagonists stimulate motor activity: evidence for an increased effectiveness in aged rats”. Neuroscience Letters 251 (3): 201–4. DOI:10.1016/S0304-3940(98)00533-3. PMID 9726378. 
  8. ↑ El Yacoubi M, Ledent C, Ménard JF, Parmentier M, Costentin J, Vaugeois JM (April 2000). „The stimulant effects of caffeine on locomotor behaviour in mice are mediated through its blockade of adenosine A(2A) receptors”. British Journal of Pharmacology 129 (7): 1465–73. DOI:10.1038/sj.bjp.0703170. PMC 1571962. PMID 10742303. 
  9. ↑ Kuzmin A, Johansson B, Gimenez L, Ogren SO, Fredholm BB (February 2006). „Combination of adenosine A1 and A2A receptor blocking agents induces caffeine-like locomotor stimulation in mice”. European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology 16 (2): 129–36. DOI:10.1016/j.euroneuro.2005.07.001. PMID 16054807. 
  10. ↑ El Yacoubi M, Costentin J, Vaugeois JM (December 2003). „Adenosine A2A receptors and depression”. Neurology 61 (11 Suppl 6): S82–7. PMID 14663017. 
  11. ↑ Monopoli A, Lozza G, Forlani A, Mattavelli A, Ongini E (December 1998). „Blockade of adenosine A2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats”. Neuroreport 9 (17): 3955–9. DOI:10.1097/00001756-199812010-00034. PMID 9875735. 
  12. ↑ Popoli P, Pintor A, Domenici MR, Frank C, Tebano MT, Pèzzola A, Scarchilli L, Quarta D, Reggio R, Malchiodi-Albedi F, Falchi M, Massotti M (March 2002). „Blockade of striatal adenosine A2A receptor reduces, through a presynaptic mechanism, quinolinic acid-induced excitotoxicity: possible relevance to neuroprotective interventions in neurodegenerative diseases of the striatum”. Journal of Neuroscience 22 (5): 1967–75. PMID 11880527. 
  13. ↑ Melani A, Gianfriddo M, Vannucchi MG, Cipriani S, Baraldi PG, Giovannini MG, Pedata F (February 2006). „The selective A2A receptor antagonist SCH 58261 protects from neurological deficit, brain damage and activation of p38 MAPK in rat focal cerebral ischemia”. Brain Research 1073-1074: 470–80. DOI:10.1016/j.brainres.2005.12.010. PMID 16443200. 
  14. ↑ Minghetti L, Greco A, Potenza RL, Pezzola A, Blum D, Bantubungi K, Popoli P (May 2007). „Effects of the adenosine A2A receptor antagonist SCH 58621 on cyclooxygenase-2 expression, glial activation, and brain-derived neurotrophic factor availability in a rat model of striatal neurodegeneration”. Journal of Neuropathology and Experimental Neurology 66 (5): 363–71. DOI:10.1097/nen.0b013e3180517477. PMID 17483693. 
  15. ↑ Canas PM, Porciúncula LO, Cunha GM, Silva CG, Machado NJ, Oliveira JM, Oliveira CR, Cunha RA (November 2009). „Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid peptides via p38 mitogen-activated protein kinase pathway”. Journal of Neuroscience 29 (47): 14741–51. DOI:10.1523/JNEUROSCI.3728-09.2009. PMID 19940169. 
  16. ↑ Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N, Schwarzschild MA (May 2001). „Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease”. Journal of Neuroscience 21 (10): RC143. PMID 11319241. 
  17. ↑ Simola N, Fenu S, Baraldi PG, Tabrizi MA, Morelli M (October 2006). „Dopamine and adenosine receptor interaction as basis for the treatment of Parkinson's disease”. Journal of the Neurological Sciences 248 (1-2): 48–52. DOI:10.1016/j.jns.2006.05.038. PMID 16780890. 

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