The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 276, Issue 2, 1996, Pages 398-404

  Zocchi, Cristina ^a   Ongini, Ennio ^a   Conti, Annamaria ^a   Monopoli, Angela ^a   Negretti, Annay ^a   Baraldi, Pier Giovanni ^b   Dionisotti, Silvio ^a  

^a Schering Plough Research Institute   (Italy)

^b UNIVERSITY OF FERRARA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; ADENOSINE RECEPTOR; ANTITHROMBOCYTIC AGENT; PYRIMIDINE DERIVATIVE; TRIAZOLE DERIVATIVE;

ANIMAL; ARTICLE; CATTLE; CORONARY BLOOD VESSEL; DRUG ANTAGONISM; DRUG EFFECT; GUINEA PIG; HEART CONTRACTION; IN VITRO STUDY; MALE; METABOLISM; PHYSIOLOGY; RABBIT; RAT; SPRAGUE DAWLEY RAT; SWINE; THROMBOCYTE AGGREGATION;

ANIMALS; CATTLE; CORONARY VESSELS; GUINEA PIGS; MALE; MYOCARDIAL CONTRACTION; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; PYRIMIDINES; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, PURINERGIC P1; SWINE; TRIAZOLES;

EID: 0030075741     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. AHN, H. S , FOSTER, M., FOSTER, C., SYBERTZ, E. AND WELLS, J. N.: Evidence for essential histidine and cysteine residues in calcium/calmodulin-sensitive cyclic nucleotide phosphodiesterase. Biochemistry 30: 6754-6760, 1991.
2. BALWIERCZAK, J. L., SHARIF, R., KRULAN, C. M., FIELD, F. P., WEISS, G. B. AND MILLER, M. J. S.: Comparative effects of a selective adenosine A2 receptor agonist, CGS 21680, and nitroprusside in vascular smooth muscle. Eur. J. Pharmacol. 196: 117-123, 1991.
3. 2a adenosine receptor antagonists. Bioorg. Med. Chem. Lett. 4: 2539-2544, 1994.
4. BORN, G. V. R. AND CROSS, M. J.: The aggregation of blood platelets. J. Physiol. (Lond.) 168: 178-195, 1963.
5. 3H] phenylxanthine. Proc. Natl. Acad. Sci. U.S.A. 77: 5547-5551, 1980.
6. 2 adenosine receptor agonists on cardiovascular tissues. Naunyn-Schmiedeberg's Arch. Pharmacol. 348: 108-112, 1993.
7. CRONING, M. D. R., GURDEN, M. F. AND KENNEDY, I.: Potencies of adenosine receptor-blocking drugs on dog isolated coronary artery and guinea-pig isolated aorta. Br. J. Pharmacol. 103: 303P, 1992.
8. 2 adenosine receptor antagonist 8FB-PTP, an 8 substituted pyrazolo-triazolo-pyrimidine, on in vitro functional models. Br. J. Pharmacol. 112: 659-665, 1994.
9. DIONISOTTI, S., ZOCCHI, C., VARANI, K., BOREA, P. A. AND ONGINI, E., Effects of adenosine derivatives on human and rabbit platelet aggregation. Correlation of adenosine receptor affinities and antiaggregatory activity. NaunynSchmiedeberg's Arch. Pharmauol. 346: 673-676, 1992.
10. 2 receptors in the neostriatum. Brain Res. 594: 124-130, 1992.
11. 2 receptors in rat striatal membranes, Proc. Natl. Acad. Sci. U.S.A. 88: 7238-7241, 1991.
12. FREDHOLM, B. B., ABBRACCHIO M. P., BURNSTOCK, G., DALY, J. W., HARDEN, T. K., JACOBSON, K. A., LEFF, P. AND WILLIAMS, M.: Nomenclature and classification of purinoceptors. Pharmaeol. Rev. 46: 143-156, 1994.
13. 2 receptor antagonist, reduces cerebral ischemic injury in the Mongolian gerbil. Life Sci. 55:61-65, 1994.
14. 2 adenosine receptor antagonists. Eur. J. Med. Chem. 28: 569-577, 1993.
15. 1-selective antagonist, DPCPX Psychopharmacology 103: 541-544, 1991.
16. GURDEN, M. F., COATES, J., ELLIS, F., EVANS, B., FOSTER, M., HORNBY, E., KENNEDY, I., MARTIN, D. P., STRONG, P., VARDEY, C. J. AND WHEELDON, A.: Functional characterization of three adenosine receptor types, Br. J. Pharmacol. 109: 693-698, 1993.
17. 2-seleetive adenosine antagonists. J. Med. Chem. 36: 1333-1342, 1993a.
18. 2-adenosine antagonist in vitro and in vivo. FEBS Lett. 323: 141-144, 1993b.
19. 2 receptors in rat brain. J. Pharmacol. Exp. Ther. 251: 888-893, 1989.
20. 2a receptor antagonist with anticataleptic activity. Eur. J Pharmaeol. 256: 263-268, 1994.
21. 3 adenosine receptors. J. Med. Chem 37: 3614-3621, 1994.
22. 2a receptor-mediated modulation of striatal GABA and ACh release. Br. J. Pharmaeol. 113: 43-48, 1994.
23. 3H]NECA binding sites by gel filtration. Naunyn-Schmiedeberg's Arch. Pharmaeol. 337: 64-68, 1988.
24. LONDOS, C., COOPER, D. M. F. AND WOLFF, J.: Subclasses of external adenosine receptors. Proc. Natl. Acad Sci. U.S.A. 77: 2551-2554, 1980.
25. 2 receptors in guinea pig aorta. J. Pharmaeol Exp. Ther 269: 1228-1235, 1994.
26. 2a adenosine receptor agonist 2-hexynyl-5′-ethylcarboxamidoadenosine. Arzneim. Forsch/Drug Res. 44: 1296-1304, 1994.
27. MUNSON, P. J. AND RODBARD, P.: LIGAND: A versatile computerized approach for characterization of ligand-brading systems. Anal. Biochem. 107: 220-239, 1980.
28. 2 receptor antagonist. Eur. J. Pharmacol. 267: 335-341, 1994.
29. 2 antagonist, (E)-1,3-dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. J. Med. Chem. 36: 3731-3733, 1993.
30. 3 adenosine receptor. Mol. Pharmacol. 45: 978-982, 1994.
31. b receptors expressed in CHO cells. Biochem. Soc. Trans. 22: 195, 1994.
32. SAS INSTITUTE INC.: SAS/STAT Guide For Personal Computer, Version 6, ed. by SAS Institute Inc., pp. 549-640 (PROC GLM), pp. 675-693 (PROC NLIN), Cary, 1987.
33. 2 antagonists. J. Med. Chem. 35: 2342-2345, 1992.
34. SIMPSON, R. E , O'REGAN, M. H., PERKINS, L. M. AND PHILLIS, J. W.: Excitatory transmitter amino acid release from the ischemic rat cerebral cortex: Effects of adenosine receptor agonists and antagonists. J. Neurochem. 58: 1683-1690, 1992.
35. VAN CALKER, D., MULLER, M. AND HAMPHBCHT, B.: Adenosine regulates via two different types of receptors the accumulation of cyclic AMP in cultured brain cells. J. Neurochem. 33: 999-1005, 1979.
36. 2 receptors: Structure function relationships. Med. Res. Rev. 12: 423-471, 1992.
37. WILLIAMS, M., FRANCIS, J., GHAI, G., BRAUNWALDER, A., PSYCHOYOS, S., STONE, G. A. AND CASH, W. D.: Biochemical characterization of the triazoloquinazoline, CGS 15943, a novel, non-xanthine adenosine antagonist. J. Pharmacol. Exp. Ther. 241: 415-420, 1987.
38. WILLIAMS, M. AND JARVIS, M. F.: Adenosine antagonists as potential therapeutic agents. Pharmacol. Biochem. Behav. 29: 433-441, 1988.
39. 3 adenosine receptor. Proc. Natl. Acad. Sci. U.S.A. 89: 7432-7436, 1992.
40. 2A adenosine receptor antagonist, to rat striatal membranes. Br. J. Pharmacol., in press.