1H-Pyrazolo[4,3-d]pyrimidine-7(6H)-one and 5H-Pyrazolo[4,3-d] 1,2,3-triazin-4(3H)-one Derivatives: Synthesis and in vitro biological activity at adenosine A1 and A2a receptors

Arzneimittel-Forschung/Drug Research

Volumn 46, Issue 4, 1996, Pages 365-368

  Baraldi, Pier G ^a   Cacciari, Barbara ^a   Dalpiaz, Alessandro ^a   Dionisotti, Silvio ^b   Zocchi, Cristina ^b   Pineda De Las Infantas, Maria J ^a   Spalluto, Giampiero ^a   Varani, Katia ^a  

^a UNIVERSITY OF FERRARA   (Italy)

^b Schering Plough   (Italy)

Author keywords

1H Pyrazolo 4,3 d pyrimidine 7(6H) ones; 5H Pyrazolo 4,3 d 1,2,3 triazin 4(3H) ones; Adenosine receptors, A1 and A2a antagonists, binding studies

Indexed keywords

1H PYRAZOLO[4,3 D]PYRIMIDINE 7(6H)ONE DERIVATIVE; 2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 5H PYRAZOLO[4,3 D] 1,2,3 TRIAZIN 4(3H)ONE DERIVATIVE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A1 RECEPTOR; ADENOSINE A2A RECEPTOR; ADENOSINE RECEPTOR; ADENOSINE RECEPTOR AFFECTING AGENT; ADENOSINE RECEPTOR BLOCKING AGENT; CYCLOHEXYLADENOSINE; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; BRAIN CORTEX; BRAIN MEMBRANE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; MALE; NONHUMAN; RAT; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

ADENOSINE; ALKYLATION; ANIMALS; BRAIN CHEMISTRY; CHEMISTRY, PHYSICAL; MAGNETIC RESONANCE SPECTROSCOPY; MALE; MEMBRANES; PHENETHYLAMINES; PYRAZOLES; PYRIMIDINES; RATS; RATS, WISTAR; RECEPTORS, PURINERGIC P1; TRIAZINES;

EID: 0029997268     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (27)

1. Fredholm, B. B., Abbracchio, M. P., Burnstock, G. et al., Pharmacol. Rev. 46, 143 (1994)
2. Muller, C. E., Scior, T., Pharm. Acta Helv. 68, 77 (1993)
3. Van Galen, P. J. M., Stiles, G. L., Michaels, G. S. et al., Res. Rev. 12, 423 (1992)
4. Kim, H. O., Ji, X., Helman, N., Olah, M. E. et al., J. Med. Chem. 37, 3373 (1994)
5. Habraken, C., Moore, J. A., J. Org. Chem. 30, 1982 (1965)
6. Hamilton, H. W., Ortwine, D. F., Worth, D. F. et al., J. Med. Chem. 28, 1071 (1985)
7. Hamilton, H. W., Ortwine, D. F., Worth, D. F., J. Med. Chem. 30, 91 (1987)
8. Baraldi, P. G., Guarneri, M., Moroder, F. et al., Synthesis 727 (1981)
9. Baraldi, P. G., Vicentini, C. B., Simoni, D. et al., Il Farmaco 38, 369 (1983)
10. Baraldi, P. G., Vincentini, C. B., Simoni, D. et al., Il Farmaco 38, 508 (1983)
11. Baraldi, P. G., Simoni, D., Periotto, V. et al., J. Med. Chem. 27, 986 (1984)
12. Baraldi, P. G., Casolari, A. Guarneri, M. et al., Synthesis 78 (1988)
13. Baraldi, P. G., Casolari, A., Manfredini, S. et al., Arzneim.-Forsch./Drug Res. 38 (II), 1262 (1988)
14. Baraldi, P. G., Garuti, L., Roberti, M., Synthesis, 1437 (1994)
15. Baraldi, P. G., Chiarini, A., Budriesi, R., Drug Design and Delivery 5, 13 (1989)
16. Borea, P. A., Varani, K., Guerra, L. et al., Mol. Neuropharmacol. 2, 273 (1992)
17. Borea, P. A., Dalpiaz, A., Varani, K. et al., Biochem. Pharmacol. 49, 461 (1995)
18. Bruns, R. F., Daly, J. W., Snyder, S. H., Proc. Natl. Acad. Sci. USA 55, 5547 (1980)
19. Jarvis, M. F., Schultz, R., Hutchison, A. J., J. Pharmacol, Exp. Ther. 251, 888 (1989)
20. Finney, D. J., Statistical Methods in Biological Assays, 3rd edn., p. 80, Griffin, London (1982)
21. Cheng, Y. C., Prusoff, H. R., Biochem. Pharmacol. 22, 3099 (1973)
22. Jacobson, K. A., Gallo-Rodriguez, C., Melmann, N. et al., J. Med. Chem. 36, 1333 (1993)
23. Nonaka, Y., Shimada, J., Nonaka, H. et al., J. Med. Chem. 36, 3731 (1993)
24. Williams, M., Jarvis, M. F., Pharmacol. Biochem. Be. 29, 433 (1988)
25. Rall, T. W., The pharmacological basis of therapeutics, 7th ed., A. G. Gilman, L. S. Goodman, T. W. Rall et al. (eds.), pp. 589-602, Macmillan Publishing Co., New York (1985)
26. Suzuki, F., Shimada, J., Mizumoto, H. et al., J. Med. Chem. 35, 3066 (1992)
27. Jacobson, K. A., van Galen, P. J. M., Wiliams, M., J. Med. Chem. 35, 407 (1992)