CGS-15943
 | |
| Clinical data | |
|---|---|
| ATC code |
|
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C13H8ClN5O |
| Molar mass | 285.69 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?) (verify) | |
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
- ^ 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. doi:10.1007/bf02244256. PMID 2062988. S2CID 23153942.
- ^ 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. S2CID 144535664.
 | This drug article relating to the cardiovascular system is a stub. You can help Wikipedia by expanding it. |
 | This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it. |