CGS-15943

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]

CGS-15943
Clinical data
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC13H8ClN5O
Molar mass285.69 g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

See also

References
  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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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