Template: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") |
16-Epiestriol • 17α-Estradiol • ent-Estradiol • 16-Ketoestradiol • Dimethylstilbestrol • meso-Butestrol
|
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. Estradiol • Estrone • Ethinylestradiol • Diethylstilbestrol • Hexestrol | Intermediate (6–24 hours) | Single or once-daily injections: full agonist | Early and late responses |
B. Clomifene • Nafoxidine • Nitromifene • Tamoxifen | 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 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]
|
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