CGS-15943 explained

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.^{[1] [2]} 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.^{[3] [4] [5] [6] [7]}

See also

• ATL-444
• SCH-58261

Notes and References

1. Williams M, Francis J, Ghai G, Braunwalder A, Psychoyos S, Stone GA, Cash WD . Biochemical characterization of the triazoloquinazoline, CGS 15943, a novel, non-xanthine adenosine antagonist . The Journal of Pharmacology and Experimental Therapeutics . 241 . 2 . 415–20 . May 1987 . 2883298 .
2. Ghai G, Francis JE, Williams M, Dotson RA, Hopkins MF, Cote DT, Goodman FR, Zimmerman MB . Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist . The Journal of Pharmacology and Experimental Therapeutics . 242 . 3 . 784–90 . September 1987 . 3656113 .
3. Holtzman SG . CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats . Life Sciences . 49 . 21 . 1563–70 . 1991 . 1943461 . 10.1016/0024-3205(91)90329-A.
4. Griebel G, Saffroy-Spittler M, Misslin R, Remmy D, Vogel E, Bourguignon JJ . 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 . 1991 . 2062988 . 10.1007/bf02244256. 23153942 .
5. Howell LL, Byrd LD . 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 . October 1993 . 8229772 .
6. Holtzman SG . 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 . May 1996 . 8627553 .
7. Weerts EM, Griffiths RR . The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons . Psychopharmacology . 168 . 1–2 . 155–63 . July 2003 . 12669180 . 10.1007/s00213-003-1410-5 . 144535664 .