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 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 Clc1cc2c3nc(nn3c(nc2cc1)N)c4occc4; ;
	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) ; Key:MSJODEOZODDVGW-UHFFFAOYSA-N ;

CGS-15943 je lek koji deluje kao potentan i selektivan antagonist adenozinskih receptora A₁ i A_2A, sa K_i od 3,3 nM na A_2A 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 уреди

^ 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.

Vidi još уреди

Spoljašnje veze уреди

[pmid2883298-1] 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.

[pmid3656113-2] 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.

[pmid1943461-3] 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.

[pmid2062988-4] 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.

[pmid8229772-5] 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.

[pmid8627553-6] 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.

[pmid12669180-7] 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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