CGS-15943: Difference between revisions

| verifiedrevid = 445988056

| image = CGS-15943_structure.png

| routes_of_administration =

| excretion =

| CAS_number = <!-- blanked - oldvalue: 104615-18-1 -->

| IUPHAR_ligand =

| molecular_weight = 285.689 g/mol

| smiles = Clc1cc2c3nc(nn3c(nc2cc1)N)c4occc4

'''CGS-15943''' is a [[drug]] which acts as a [[potency (pharmacology)|potent]] and reasonably selective [[receptor antagonist|antagonist]] for the [[adenosine]] [[Receptor (biochemistry)|receptor]]s [[Adenosine A1 receptor|A₁]] and [[Adenosine A2A receptor|A_2A]], having a [[Dissociation constant#Protein-ligand binding|K_i]] of 3.3nM at A_2A and 21nM at A₁. It was one of the first [[adenosine receptor]] antagonists discovered that is not a [[xanthine]] derivative, instead being a triazoloquinazoline.<ref name="pmid2883298">{{cite journal |author=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 |pages=415–20 |year=1987 |month=May |pmid=2883298 |doi= |url=}}</ref><ref name="pmid3656113">{{cite journal |author=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 |pages=784–90 |year=1987 |month=September |pmid=3656113 |doi= |url=}}</ref> Consequently CGS-15943 has the advantage over most xanthine derivatives that it is not a [[phosphodiesterase inhibitor]], and so has more a specific pharmacological effects profile. It produces similar effects to [[caffeine]] in animal studies, though with higher potency.<ref name="pmid1943461">{{cite journal |author=Holtzman SG |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 |pages=1563–70 |year=1991 |pmid=1943461 |doi= 10.1016/0024-3205(91)90329-A|url=}}</ref><ref name="pmid2062988">{{cite journal |author=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 |pages=541–4 |year=1991 |pmid=2062988 |doi= |url=}}</ref><ref name="pmid8229772">{{cite journal |author=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 |pages=432–9 |year=1993 |month=October |pmid=8229772 |doi= |url=}}</ref><ref name="pmid8627553">{{cite journal |author=Holtzman SG |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 |pages=739–46 |year=1996 |month=May |pmid=8627553 |doi= |url=}}</ref><ref name="pmid12669180">{{cite journal |author=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 |pages=155–63 |year=2003 |month=July |pmid=12669180 |doi=10.1007/s00213-003-1410-5 |url=}}</ref>

{{Stimulants}}

[[Category:Receptor antagonists]]