CGS-15943

CGS-15943
Clinical data
ATC code	none;
Legal status
Legal status	In general: uncontrolled;
Identifiers
	IUPAC name 9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;
CAS Number	104615-18-1 ;
PubChem CID	2690;
IUPHAR/BPS	384;
ChemSpider	2589 ;
UNII	Y5A5D5E2AQ;
ChEBI	CHEBI:131351 ;
ChEMBL	ChEMBL16687 ;
CompTox Dashboard (EPA)	DTXSID80146617 ;
Chemical and physical data
Formula	C13H8ClN5O
Molar mass	285.69 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES ClC1=CC=C2N=C(N)N3N=C(C4=CC=CO4)N=C3C2=C1;
	InChI InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16) ; Key:MSJODEOZODDVGW-UHFFFAOYSA-N ;
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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]

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.

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[pmid2883298-1] 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.

[pmid3656113-2] 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.

[pmid1943461-3] 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.

[pmid2062988-4] 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. S2CID 23153942.

[pmid8229772-5] 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.

[pmid8627553-6] 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.

[pmid12669180-7] 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. S2CID 144535664.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

Clinical data

ATC code	none
Legal status
Legal status	In general: uncontrolled
Identifiers
IUPAC name 9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
CAS Number	104615-18-1^Y
PubChem CID	2690
IUPHAR/BPS	384
ChemSpider	2589^Y
UNII	Y5A5D5E2AQ
ChEBI	CHEBI:131351^N
ChEMBL	ChEMBL16687^Y
CompTox Dashboard (EPA)	DTXSID80146617
Chemical and physical data
Formula	C₁₃H₈ClN₅O
Molar mass	285.69 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES ClC1=CC=C2N=C(N)N3N=C(C4=CC=CO4)N=C3C2=C1
InChI InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)^Y Key:MSJODEOZODDVGW-UHFFFAOYSA-N^Y
^NY (what is this?) (verify)

CGS-15943

See also

References