Template:Classification of estrogens and antiestrogens by receptor–estrogen complex retention

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Classification of estrogens and antiestrogens by receptor–estrogen complex retention

Class Examples RE complex retention Pharmacodynamic profile Uterine effects
Short-acting (a.k.a.
"weak" or "impeded")
Template:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflink Short (1–4 hours) Single or once-daily injections: partial agonist or antagonist Early responsesa
Implant or multiple injections per day: full agonist Early and late responsesb
Long-acting A. Template:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflink Intermediate (6–24 hours) Single or once-daily injections: full agonist Early and late responses
B. Template:No selflinkTemplate:No selflinkTemplate:No selflinkTemplate:No selflink Long (>24–48 hours) Single injection: agonist
Repeated injections: antagonist
Early and late responses
Footnotes: a = Early responses occur after 0–6 hours and include water imbibition, hyperemia, amino acid and nucleotide uptake, activation of RNA polymerases I and II, and stimulation of induced protein, among others. b = Late responses occur after 6–48 hours and include cellular hypertrophy and hyperplasia and sustained RNA polymerase I and II activity, among others. Sources: [1][2][3][4][5][6][7]
Template documentation

See also

References

  1. Clark JH, Paszko Z, Peck EJ (January 1977). "Nuclear binding and retention of the receptor estrogen complex: relation to the agonistic and antagonistic properties of estriol". Endocrinology. 100 (1): 91–6. doi:10.1210/endo-100-1-91. PMID 830547.
  2. Clark JH, Hardin JW, McCormack SA (1979). "Mechanism of action of estrogen agonists and antagonists". J. Anim. Sci. 49 Suppl 2: 46–65. doi:10.1093/ansci/49.supplement_ii.46. PMID 400777.
  3. Lunan CB, Klopper A (September 1975). "Antioestrogens. A review". Clin. Endocrinol. (Oxf). 4 (5): 551–72. doi:10.1111/j.1365-2265.1975.tb01568.x. PMID 170029.
  4. Rabe, T.; Runnebaum, B.; Kellermeier-Wittlinger, S. (1994). "Hormontherapie" [Hormone Therapy]. In Benno Runnebaum; Thomas Rabe (eds.). Gynäkologische Endokrinologie und Fortpflanzungsmedizin: Band 1: Gynäkologische Endokrinologie [Gynecological Endocrinology and Reproductive Medicine: Volume 1: Gynecological Endocrinology]. pp. 63–147. doi:10.1007/978-3-662-07635-4_3. ISBN 978-3-662-07635-4.
  5. Clark JH, Markaverich BM (1983). "The agonistic and antagonistic effects of short acting estrogens: a review". Pharmacol. Ther. 21 (3): 429–53. doi:10.1016/0163-7258(83)90063-3. PMID 6356176.
  6. Clark JH, Markaverich BM (April 1984). "The agonistic and antagonistic actions of estriol". J. Steroid Biochem. 20 (4B): 1005–13. doi:10.1016/0022-4731(84)90011-6. PMID 6202959.
  7. Terenius L, Ljungkvist I (1972). "Aspects on the mode of action of antiestrogens and antiprogestogens". Gynecol Invest. 3 (1): 96–107. doi:10.1159/000301746. PMID 4347201.