|
}}
-{'''CGS-15943'''}- je [[lek]] koji deluje kao [[Potentnost (farmakologija)|potentan]] i selektivan [[antagonist (farmakologija)|antagonist]] [[adenozin]]skih [[Receptor (biohemija)|receptora]] [[Adenozinski A1 receptor|A<sub>1</sub>]] i [[Adenozinski A2A receptor|A<sub>2A</sub>]], sa [[Konstanta disocijacije|-{K<sub>i</sub>}-]] od 3,3 -{nM}- na -{A<sub>2A</sub>}- i 21 -{nM}- na A<sub>1</sub>. On je bio jedan od prvih antagonista [[adenozinski receptor|adenozinskog receptora]] koji nije derivat [[ksantin]]a, već je triazolohinazolin.<ref name="pmid2883298">{{cite journal |vauthors=Williams M, Francis J, Ghai G, Braunwalder A, Psychoyos S, Stone GA, Cash WD |title=Biochemical characterization of the triazoloquinazoline, CGS 15943, a novel, non-xanthine adenosine antagonist |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=241 |issue=2 |year=1987|month=May |pmid=2883298 |doi= |url=|pages=415–20}}</ref><ref name="pmid3656113">{{cite journal |vauthors=Ghai G, Francis JE, Williams M, Dotson RA, Hopkins MF, Cote DT, Goodman FR, Zimmerman MB |title=Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=242 |issue=3 |year=1987|month=September |pmid=3656113 |doi= |url=|pages=784–90}}</ref> 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 [[kofein]]om u životinjskim studijama, mada se većom potencijom.<ref name="pmid1943461">{{cite journal |last=SG|first=Holtzman|title=CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats |journal=Life Sciences |volume=49 |issue=21 |year=1991|pmid=1943461 |doi= 10.1016/0024-3205(91)90329-A|url=|pages=1563–70}}</ref><ref name="pmid2062988">{{cite journal |vauthors=Griebel G, Saffroy-Spittler M, Misslin R, Remmy D, Vogel E, Bourguignon JJ |title=Comparison of the behavioural effects of an adenosine A1/A2-receptor antagonist, CGS 15943A, and an A1-selective antagonist, DPCPX |journal=Psychopharmacology |volume=103 |issue=4 |year=1991|pmid=2062988 |doi= |url=|pages=541–4}}</ref><ref name="pmid8229772">{{cite journal |vauthors=Howell LL, Byrd LD |title=Effects of CGS 15943, a nonxanthine adenosine antagonist, on behavior in the squirrel monkey |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=267 |issue=1 |year=1993|month=October |pmid=8229772 |doi= |url=|pages=432–9}}</ref><ref name="pmid8627553">{{cite journal |last=SG|first=Holtzman|title=Discriminative effects of CGS 15943, a competitive adenosine receptor antagonist, in monkeys: comparison to methylxanthines |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=277 |issue=2 |year=1996|month=May |pmid=8627553 |doi= |url=|pages=739–46}}</ref><ref name="pmid12669180">{{cite journal |vauthors=Weerts EM, Griffiths RR |title=The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons |journal=Psychopharmacology |volume=168 |issue=1-2 |year=2003|month=July |pmid=12669180 |doi=10.1007/s00213-003-1410-5 |url=|pages=155–63}}</ref>
== Reference ==
|
