Structure Activity Relationships for Adenosine Agonists

  • B. K. Trivedi


Adenosine elicits a wide variety of physiological responses (Williams, 1987) via interactions with two major subtypes of extracellular adenosine receptors, designated as A1 and A2. These two receptor subtypes can be distinguished on the basis of structure-activity relationships (Hamprecht et al., 1985) and have opposite effects on adenylate cyclase (Londos et al., 1980). With the advent of an A2 binding assay (Bruns et al., 1986, Yeung et al., 1984), it has become possible to quantitatively evaluate the subtype selectivity of adenosine agonists. Recently, considerable effort has been devoted to the search for adenosine agonists with high selectivity for either A1 or A2 receptors. Our interest in adenosine receptors began with earlier disclosures that adenosine agonists such as R-PIA (Snyder et al., 1981), NECA (Prasad et al., 1980) or CV-1808 (Kawazoe et al., 1980) had potential utility as therapeutic agents (Figure 1). Thus, we set, out to develop structure-activity relationships (SAR) for both A1 and A2 receptors and especially to identify receptor selective agonists.


Adenosine Receptor Pharmacophore Model Adenosine Agonist Sulfone Derivative Receptor Selective Agonist 
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  1. Bridges, A.J., 1989, Nucleosides and Nucleotides 8(3):357.CrossRefGoogle Scholar
  2. Bridges, A.J., Moos, W.H., Szotek, D.L., Trivedi, B.K., Bristol, J.A., Heffner, T.G., Bruns, R.F., Downs, D.A., 1987, J. Med. Chem. 30:1709.PubMedCrossRefGoogle Scholar
  3. Bridges, A. J., Bruns, R. F., Ortwine, D. F., Priebe, S. R., Szotek, D. L., Trivedi, B. K., 1988, J. Med. Chem. 31:1282.PubMedCrossRefGoogle Scholar
  4. Bruns, R. F., Lu, G. H., Pugsley, T. A., 1986, Mol. Pharmacol. 29:331.PubMedGoogle Scholar
  5. Daly, J. W., Padgett, W., Thompson, R. D., Kusachi, S., Bugni, W. J., Olsson, R. A., 1986, Biochem. Pharmacol. 35:2467.PubMedCrossRefGoogle Scholar
  6. Hamprecht, B., van Calker, D., 1985, Trends Pharmacol. Sci. 6:153.CrossRefGoogle Scholar
  7. Kawazoe, K., Matsumoto, N., Tanabe, N., Fujiwara, S., Yanajimoto, M., Hirata, M., Kikuchi, K., 1980, Arzneim.-Forsch. 30:1083.Google Scholar
  8. Londos, C., Cooper, D. M. F., Wolff, J., 1980, Proc. Natl. Acad. Sci. U.S.A. 77:2551.PubMedCrossRefGoogle Scholar
  9. Marumoto, R., Yoshikoto, Y., Miyashita, O., Shima, S., Imai, K., Kawazoe, K., Honjo, M., 1975, Chem. Pharm. Bull. 23:759.PubMedGoogle Scholar
  10. Marumoto, R., Omura, K., Furukawa, Y., 1981, Chem. Pharm. Bull. 29:1870.Google Scholar
  11. Moos, W. H., Szotek, D. L., Bruns, R. F., 1985, J. Med. Chem. 28:1383.PubMedCrossRefGoogle Scholar
  12. Ortwine, D. F., Bridges, A. J., Humblet, C., Trivedi, B. K., 1990, see chapter in this book.Google Scholar
  13. Prasad, R. N., Bariana, D. S., Fung, A., Savic, M., Tietje, K., Stein, H. H., Brondyk, H., Egan, R. S., 1980, J. Med. Chem. 23:313.PubMedCrossRefGoogle Scholar
  14. Snyder, S. H., Katims, J. J., Annau, Z., Bruns, R. F., Daly, J. W., 1981, Proceedings of the National Academy of Sciences USA 78:3260.CrossRefGoogle Scholar
  15. Trivedi, B. K., Bristol, J. A., Bruns, R. F., Haleen, S. J., Steffen, R. P., 1988, J. Med. Chem. 31:271.PubMedCrossRefGoogle Scholar
  16. Trivedi, B. K., 1988, Nucleosides and Nucleotides 7:393.CrossRefGoogle Scholar
  17. Trivedi, B. K., Bridges, A. J., Patt, W. C., Priebe, S. R., Bruns, R. F., 1989, J. Med. Chem. 32:8.PubMedCrossRefGoogle Scholar
  18. Trivedi, B. K., Bruns, R. F., 1989, J. Med. Chem. 32:1667.PubMedCrossRefGoogle Scholar
  19. Williams, M., 1987, Annu. Rev. Pharmacol. 27:315.CrossRefGoogle Scholar
  20. Yeung, S. M. H., Green, R. D., 1984, Naunyn-Schmiedeberg’s Arch. Pharmacol. 325:218.CrossRefGoogle Scholar

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© Springer-Verlag New York Inc. 1990

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  • B. K. Trivedi

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