Steroid hormones—agonists and antagonists

  • J. P. Raynaud
  • T. Ojasoo
  • F. Labrie
Part of the Biological Council The Co-ordinating Committee for Symposia on Drug Action book series


Steroid hormones are frequently classified into broad categories such as ‘progestins’, ‘androgens’ and ‘glucocorticoids’, but this classification is often misleading or just incomplete since it only accounts for their known primary biological activity and does not adequately describe the multiplicity of actions that many of them display. In view of the ubiquity of the receptors of different classes of steroid hormone (for instance, each of the oestrogen, progestin, androgen and glucocorticoid receptors has been identified in peripheral target tissues such as the uterus and pituitary and in central tissues such as the hypothalamus), it is of interest to be able to define the receptor binding profile of a new substance and thus extrapolate, by comparison with the natural hormones and well-established steroid drugs, the possible actions of this new compound in different organs. Furthermore, since interdependent regulatory mechanisms seem to condition many hormonal responses (for example, both progestin and androgen binding sites can be induced by oestrogens), it is useful to know whether certain potent drugs classified as agonists of one natural hormone are antagonists of another.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Agarwal, M. K. and Paillard, J. (1979). Biochem. biophys. Res. Commun., 89, 77–84CrossRefGoogle Scholar
  2. Albin, J., Vittek, J., Gordon, G. G., Altman, K., Olivo, J. and Southren, A. L. (1973). Endocrinology, 93, 417–422CrossRefGoogle Scholar
  3. Bell, P. A. and Jones, T. R. (1979). In: Anti-Hormones (ed. M. K. Agarwal), Elsevier/North-Holland Biomedical Press, Amsterdam, pp. 35–50Google Scholar
  4. Bhakoo, H. S. and Katzenellenbogen, B. S. (1977). Molec. cell. Endocr., 8, 121–134CrossRefGoogle Scholar
  5. Bouton, M. M. and Raynaud, J. P. (1979). Endocrinology, 105, 509–515CrossRefGoogle Scholar
  6. Brown, T. R., Bullock, L. and Bardin, C. W. (1979). Endocrinology, 105, 1281–1287CrossRefGoogle Scholar
  7. Bullock, L. P. and Bardin, C. W. (1977). Ann. N.Y. Acad. Sci., 286, 321–330CrossRefGoogle Scholar
  8. Chamness, G. C., Asch, R. H. and Pauerstein, C. J. (1980). Am. J. Obstet. Gynecol., 136, 426–429Google Scholar
  9. Clark, J. H., Paszko, Z. and Peck, E. J. Jr (1977). Endocrinology, 100, 91–96CrossRefGoogle Scholar
  10. Dausse, J. P., Duval, D., Meyer, P., Gaignault, J. C., Marchandeau, C. and Raynaud, J. P. (1977). Molec. Pharmac., 13, 948–955Google Scholar
  11. Diamondstone, T. I. (1966). Analyt. Biochem., 16, 395–401CrossRefGoogle Scholar
  12. Disorbo, D., Rosen, F., McPartland, R. P. and Milholland, R. J. (1977). Ann. N. Y. Acad. Sci., 286, 355–368CrossRefGoogle Scholar
  13. Drouin, J. and Labrie, F. (1976). Endocrinology, 98, 1528–1534CrossRefGoogle Scholar
  14. Duncan, M. R. and Duncan, G. R. (1979). J. Steroid Biochem., 10, 245–259CrossRefGoogle Scholar
  15. Funder, J. W. (1979). J. Steroid Biochem., 11, 87–91CrossRefGoogle Scholar
  16. Hackney, J. F. (1979). Pharmacologist, 21, 228.Google Scholar
  17. Hermann, W. M. and Beach, R. C. (1978). Postgrad. med. J., 54 (suppl. 2), 82–87Google Scholar
  18. Kaiser, N., Mayer, M., Milholland, R. J. and Rosen, F. (1979). J. Steroid Biochem., 10, 379–386CrossRefGoogle Scholar
  19. Labrie, F., Ferland, L., Lagacé, L., Drouin, J., Asselin, J., Azadian-Boulanger, G. and Raynaud, J. P. (1977). Fert. Steril., 28, 1104–1112Google Scholar
  20. Lerner, L. J. (1964). Rec. Prog. Horm. Res., 20, 435–490Google Scholar
  21. McKinney, G. R. and Braselton, J. P. (1970). Steroids, 15, 405–411CrossRefGoogle Scholar
  22. Miller, B. G., Wild, J. and Stone, G. M. (1979). Aust. J. biol. Sci., 32, 549–560Google Scholar
  23. Naylor, P. H., Milholland, R. J., Gilani, S. S. H. and Rosen, F. (1979). 61st Annual Meeting of the Endocrine Society, Abstr no. 620Google Scholar
  24. Nédélec, L., Torelli, V., Rousseau, G., Allais, A., Philibert, D., Fournex, R. and Azadian-Boulanger, G. (1978). J. Steroid Biochem., 9, 814–815CrossRefGoogle Scholar
  25. Neumann, F. (1977). Horm. Metab. Res., 9, 1–13CrossRefGoogle Scholar
  26. Ojasoo, T. and Raynaud, J. P. (1978). Cancer Res., 38, 4186–4198Google Scholar
  27. Raynaud, J. P. (1979). In Advances in Pharmacology and Therapeutics, vol. 1, Receptors, (ed. J. Jacob), Pergamon Press, Oxford, pp. 259–278Google Scholar
  28. Raynaud, J. P. and Bercovici, J. P. (1979). Ann. Endocr. (Paris), 40, 300–320Google Scholar
  29. Raynaud, J. P., Bonne, C., Bouton, M. M., Lagacé, L. and Labrie, F. (1979a). J. Steroid Biochem., 11, 93–99CrossRefGoogle Scholar
  30. Raynaud, J. P. and Bouton, M. M. (1980). In Cytotoxic Estrogens in Hormone Receptive Tumors (ed. J. Raus, H. Martens and G. Leclercq), Academic Press, New York, pp. 49–70Google Scholar
  31. Raynaud, J. P., Bouton, M. M. and Martin, P. M. (1980a). In Steroid Receptors, Metabolism and Prostatic Cancer (ed. F. H. Schröder and H. J. de Voogt), Excerpta Medica, Amsterdam, pp. 165–181Google Scholar
  32. Raynaud, J. P., Bouton, M. M., Moguilewsky, M., Ojasoo, T., Philibert, D., Beck, G., Labrie, F. and Mornon, J. P. (1980b). J. Steroid Biochem., 12, 143–158CrossRefGoogle Scholar
  33. Raynaud, J. P., Bouton, M. M. and Ojasoo, T. (1980c). Trends. pharmac. Sci., 1, 324–327CrossRefGoogle Scholar
  34. Raynaud, J. P., Ojasoo, T., Bouton, M. M. and Philibert, D. (1979). In Drug Design Vol. VIII, (ed. E. J. Ariens), Academic Press, New York, pp. 169–214CrossRefGoogle Scholar
  35. Raynaud, J. P., Ojasoo, T. and Vaché, V. In Traité de Gynécologie Endocrinienne (ed. P. Mauvais-Jarvis), Flammarion, Paris, in pressGoogle Scholar
  36. Reel, J. R., Humphrey, R. R., Shih, Y-H, Windsor, B. L., Sakowski, R., Creger, P. L. and Edgren, R. A. (1979). Fertil. Steril., 31, 552–561Google Scholar
  37. Rosner, J. M., Macome, J. C., Denari, J. H. and De Carli, D. N. (1972). Acta endocr. 69, 403–409Google Scholar
  38. Salmon, J., Raynaud, J. P. and Pottier, J. (1971). In Symposium sur les Progrès des Techniques Nucléaires en Pharmacodynamie, Saclay, 1970, (ed. G. Valette and Y. Cohen), Masson & Cie, Paris, pp. 237–247Google Scholar
  39. Teutsch, G. and Bélanger, A. (1979). Tetrahedron Lett., 22, 2051–2054CrossRefGoogle Scholar
  40. Trachtenberg, J., Hicks, L. L. and Walsh, P. C. (1980). J. clin. Invest., 65, 1051–1059CrossRefGoogle Scholar
  41. Wambach, G. and Higgins, J. R. (1978). Endocrinology, 102, 1686–1693CrossRefGoogle Scholar
  42. Wambach, G., Higgins, J. R., Kern, D. C. and Kaufmann, W. (1979). Acta endocr. (Kbh), 92, 560–567Google Scholar
  43. Yeakley, J. and Harrison, R. W. (1979). Fedn Proc., 38, no. 1336Google Scholar

Copyright information

© Institute of Biology Endowment Trust Fund 1981

Authors and Affiliations

  • J. P. Raynaud
    • 1
  • T. Ojasoo
    • 1
  • F. Labrie
    • 2
  1. 1.Roussel-UclafParisFrance
  2. 2.Department of Molecular EndocrinologyLe Centre Hospitalier de l’Université LavalQuébecCanada

Personalised recommendations