CGS-15943
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IUPAC ime | |
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9-hloro-2-(furan-2-il)-[1,2,4]triazolo[1,5-c]hinazolin-5-amin | |
Pravni status | |
Pravni status |
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Identifikatori | |
CAS broj | 104615-18-1 ![]() |
ATC kod | none |
PubChem | CID 2690 |
ChemSpider | 2589 ![]() |
ChEMBL | CHEMBL16687 |
Hemijski podaci | |
Formula | C13H8ClN5O |
Molarna masa | 285,689 g/mol |
SMILES
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InChI
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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
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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 (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.
- ^ 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.
- ^ 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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Antagonisti | 8-Fenil-1,3-dipropilksantin • Acefilin • Aminofilin • Bamifilin • Kofein • CGS-15943 • 8-Hloroteofilin • CPX • CVT-6883 • Dimetazan • DPCPX • Fenetilin • Istradefilin • KF-26777 • MRE3008F20 • MRS-1220 • MRS-1334 • MRS-1706 • MRS-1754 • MRS-3777 • Paraksantin • Pentoksifilin • Preladenant • Propentofilin • PSB-10 • PSB-11 • PSB 36 • PSB-603 • PSB-788 • PSB-1115 • Rolofilin • SCH-442,416 • SCH-58261 • Teobromin • Teofilin • VUF-5574 • ZM-241,385 |
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