Википедија

SCH-58261

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.[1] 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.[2][3][4][5] Takođe je pokazano da SCH-58261 ima antidepresivno[6] i neuroprotektivno dejstvo u nizu modela na životinjama,[7][8][9][10][11] i on je istraživan kao mogući tretman za Parkinsonovu bolest.[12][13]

SCH-58261
IUPAC ime
5-Amino-7-(2-feniletil)-2-(2-furil)-pirazolo(4,3-e)-1,2,4-triazolo(1,5-c)pirimidin
Pravni status
Pravni status
  • nije kontrolisan
Identifikatori
CAS broj160098-96-4 ДаY
ATC kodnone
PubChemCID 176408
IUPHAR/BPS403
ChemSpider153647 ДаY
ChEMBLCHEMBL17127 ДаY
Hemijski podaci
FormulaC18H15N7O
Molarna masa345,357 g/mol
  • n1n3c(nc4c(c3nc1c2occc2)cnn4CCc5ccccc5)N
  • InChI=1S/C18H15N7O/c19-18-22-16-13(11-20-24(16)9-8-12-5-2-1-3-6-12)17-21-15(23-25(17)18)14-7-4-10-26-14/h1-7,10-11H,8-9H2,(H2,19,22) ДаY
  • Key:UTLPKQYUXOEJIL-UHFFFAOYSA-N ДаY

Reference уреди

  1. ^ Zocchi C, Ongini E, Conti A, Monopoli A, Negretti A, Baraldi PG, Dionisotti S (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. 
  2. ^ Svenningsson P, Nomikos GG, Ongini E, Fredholm BB (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. PMID 9219939. doi:10.1016/S0306-4522(97)00046-8. 
  3. ^ Popoli P, Reggio R, Pèzzola A, Fuxe K, Ferré S (1998). „Adenosine A1 and A2A receptor antagonists stimulate motor activity: evidence for an increased effectiveness in aged rats”. Neuroscience Letters. 251 (3): 201—4. PMID 9726378. doi:10.1016/S0304-3940(98)00533-3. 
  4. ^ El Yacoubi M, Ledent C, Ménard JF, Parmentier M, Costentin J, Vaugeois JM (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. PMC 1571962  . PMID 10742303. doi:10.1038/sj.bjp.0703170. 
  5. ^ Kuzmin A, Johansson B, Gimenez L, Ogren SO, Fredholm BB (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. PMID 16054807. doi:10.1016/j.euroneuro.2005.07.001. 
  6. ^ El Yacoubi M, Costentin J, Vaugeois JM (2003). „Adenosine A2A receptors and depression”. Neurology. 61 (11 Suppl 6): S82—7. PMID 14663017. 
  7. ^ Monopoli A, Lozza G, Forlani A, Mattavelli A, Ongini E (1998). „Blockade of adenosine A2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats”. Neuroreport. 9 (17): 3955—9. PMID 9875735. doi:10.1097/00001756-199812010-00034. 
  8. ^ 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 (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. 
  9. ^ Melani A, Gianfriddo M, Vannucchi MG, Cipriani S, Baraldi PG, Giovannini MG, Pedata F (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. PMID 16443200. doi:10.1016/j.brainres.2005.12.010. 
  10. ^ Minghetti L, Greco A, Potenza RL, Pezzola A, Blum D, Bantubungi K, Popoli P (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. PMID 17483693. doi:10.1097/nen.0b013e3180517477. 
  11. ^ Canas PM, Porciúncula LO, Cunha GM, Silva CG, Machado NJ, Oliveira JM, Oliveira CR, Cunha RA (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. PMID 19940169. doi:10.1523/JNEUROSCI.3728-09.2009. 
  12. ^ Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N, Schwarzschild MA (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. 
  13. ^ Simola N, Fenu S, Baraldi PG, Tabrizi MA, Morelli M (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. PMID 16780890. doi:10.1016/j.jns.2006.05.038. 

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