CGS-15943

Из Википедије, слободне енциклопедије
CGS-15943
(IUPAC) ime
9-hloro-2-(furan-2-il)-[1,2,4]triazolo[1,5-c]hinazolin-5-amin
Klinički podaci
Identifikatori
CAS broj 104615-18-1
ATC kod nije dodeljen
PubChem[1][2] 2690
ChemSpider[3] 2589
ChEMBL[4] CHEMBL16687
Hemijski podaci
Formula C13H8ClN5O 
Mol. masa 285,689 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status nije kontrolisan

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.[5][6] 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.[7][8][9][10][11]

Reference[уреди]

  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. ^ Williams M, Francis J, Ghai G, Braunwalder A, Psychoyos S, Stone GA, Cash WD (May 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. 
  6. ^ Ghai G, Francis JE, Williams M, Dotson RA, Hopkins MF, Cote DT, Goodman FR, Zimmerman MB (September 1987). „Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist“. The Journal of Pharmacology and Experimental Therapeutics 242 (3): 784–90. PMID 3656113. 
  7. ^ Holtzman SG (1991). „CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats“. Life Sciences 49 (21): 1563–70. DOI:10.1016/0024-3205(91)90329-A. PMID 1943461. 
  8. ^ 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. 
  9. ^ Howell LL, Byrd LD (October 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. 
  10. ^ Holtzman SG (May 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. 
  11. ^ Weerts EM, Griffiths RR (July 2003). „The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons“. Psychopharmacology 168 (1-2): 155–63. DOI:10.1007/s00213-003-1410-5. PMID 12669180. 

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