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 |
InChI | 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) Y Key: MSJODEOZODDVGW-UHFFFAOYSA-N Y | |
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
- ↑ 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.
- ↑ 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
- ↑ 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
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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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