CGS-15943

{{Short description|Chemical compound}}

{{Drugbox

| Verifiedfields = changed

| Watchedfields = changed

| verifiedrevid = 459989149

| IUPAC_name = 9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine

| image = CGS-15943 Structure.svg

| tradename =

| pregnancy_category =

| legal_status = Uncontrolled

| routes_of_administration =

| bioavailability =

| metabolism =

| excretion =

| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 104615-18-1

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = Y5A5D5E2AQ

| ATC_prefix = none

| ATC_suffix =

| ChEMBL_Ref = {{ebicite|correct|EBI}}

| ChEMBL = 16687

| ChEBI_Ref = {{ebicite|changed|EBI}}

| ChEBI = 131351

| PubChem = 2690

| IUPHAR_ligand = 384

| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}

| ChemSpiderID = 2589

| C=13 | H=8 | Cl=1 | N=5 | O=1

| smiles = ClC1=CC=C2N=C(N)N3N=C(C4=CC=CO4)N=C3C2=C1

| StdInChI_Ref = {{stdinchicite|correct|chemspider}}

| StdInChI = 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)

| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}

| StdInChIKey = MSJODEOZODDVGW-UHFFFAOYSA-N

| melting_point =

| melting_high =

}}

CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A₁ and A_2A, having a 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.{{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 |pages=415–20 |date=May 1987 |pmid=2883298 }}{{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 |pages=784–90 |date=September 1987 |pmid=3656113 }} 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.{{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}}{{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 |pages=541–4 |year=1991 |pmid=2062988 |doi= 10.1007/bf02244256|s2cid=23153942 }}{{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 |pages=432–9 |date=October 1993 |pmid=8229772 }}{{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 |date=May 1996 |pmid=8627553 }}{{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 |pages=155–63 |date=July 2003 |pmid=12669180 |doi=10.1007/s00213-003-1410-5 |s2cid=144535664 }}