CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A, having a Ki of 3.3nM at A2A 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]
[edit] See also
[edit] References
- ^ 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.
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