CGS-15943

CGS-15943
IUPAC ime
9-hloro-2-(furan-2-il)-[1,2,4]triazolo[1,5-c]hinazolin-5-amin
Pravni status
Pravni status
  • nije kontrolisan
Identifikatori
CAS broj104615-18-1 ДаY
ATC kodnone
PubChemCID 2690
ChemSpider2589 ДаY
ChEMBLCHEMBL16687
Hemijski podaci
FormulaC13H8ClN5O
Molarna masa285,689 g/mol
  • Clc1cc2c3nc(nn3c(nc2cc1)N)c4occc4
  • InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16) ДаY
  • Key:MSJODEOZODDVGW-UHFFFAOYSA-N ДаY

CGS-15943 je lek koji deluje kao potentan i selektivan antagonist adenozinskih receptora A1 i A2A, sa Ki od 3,3 nM na A2A i 21 nM na A1. On je bio jedan od prvih antagonista adenozinskog receptora koji nije derivat ksantina, već je triazolohinazolin.[1][2] Konsekventno CGS-15943 ima prednost u odnosu na većinu derivata ksantina da nije inhibitor fosfodiesteraze, tako da ima specifičniji farmakološki profil. On proizvodi slične efekte sa kofeinom u životinjskim studijama, mada se većom potencijom.[3][4][5][6][7]

Reference

  1. ^ Williams M, Francis J, Ghai G, Braunwalder A, Psychoyos S, Stone GA, Cash WD (1987). „Biochemical characterization of the triazoloquinazoline, CGS 15943, a novel, non-xanthine adenosine antagonist”. The Journal of Pharmacology and Experimental Therapeutics. 241 (2): 415—20. PMID 2883298. 
  2. ^ Ghai G, Francis JE, Williams M, Dotson RA, Hopkins MF, Cote DT, Goodman FR, Zimmerman MB (1987). „Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist”. The Journal of Pharmacology and Experimental Therapeutics. 242 (3): 784—90. PMID 3656113. 
  3. ^ SG, Holtzman (1991). „CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats”. Life Sciences. 49 (21): 1563—70. PMID 1943461. doi:10.1016/0024-3205(91)90329-A. 
  4. ^ Griebel G, Saffroy-Spittler M, Misslin R, Remmy D, Vogel E, Bourguignon JJ (1991). „Comparison of the behavioural effects of an adenosine A1/A2-receptor antagonist, CGS 15943A, and an A1-selective antagonist, DPCPX”. Psychopharmacology. 103 (4): 541—4. PMID 2062988. 
  5. ^ Howell LL, Byrd LD (1993). „Effects of CGS 15943, a nonxanthine adenosine antagonist, on behavior in the squirrel monkey”. The Journal of Pharmacology and Experimental Therapeutics. 267 (1): 432—9. PMID 8229772. 
  6. ^ SG, Holtzman (1996). „Discriminative effects of CGS 15943, a competitive adenosine receptor antagonist, in monkeys: comparison to methylxanthines”. The Journal of Pharmacology and Experimental Therapeutics. 277 (2): 739—46. PMID 8627553. 
  7. ^ Weerts EM, Griffiths RR (2003). „The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons”. Psychopharmacology. 168 (1-2): 155—63. PMID 12669180. doi:10.1007/s00213-003-1410-5. 

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