CGS-15943

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	2690
ChemSpider	2589
ChEMBL	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) ; Key: MSJODEOZODDVGW-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	nije kontrolisan

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.^[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.

Povezano

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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

[pmid2883298-5] 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.

[pmid3656113-6] 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.

[pmid1943461-7] 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.

[pmid2062988-8] 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.

[pmid8229772-9] 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.

[pmid8627553-10] 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.

[pmid12669180-11] 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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