Chemistry:CGS-15943
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Short description: Chemical compound
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| Formula | C13H8ClN5O |
| Molar mass | 285.69 g·mol−1 |
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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]
See also
References
- ↑ "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. PMID 2883298.
- ↑ "Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist". The Journal of Pharmacology and Experimental Therapeutics 242 (3): 784–90. September 1987. 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.
- ↑ "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. doi:10.1007/bf02244256. PMID 2062988.
- ↑ "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. 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.
- ↑ "The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons". Psychopharmacology 168 (1–2): 155–63. July 2003. doi:10.1007/s00213-003-1410-5. PMID 12669180.
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