模板:雌激素酯和醚對雌激素受體的親和力和雌激素效價強度
雌激素 | Other names | RBA (%)a | REP (%)b | |||
---|---|---|---|---|---|---|
ER | ERα | ERβ | ||||
雌二醇 | E2 | 100 | 100 | 100 | ||
3-硫酸雌二醇 | E2S、E2-3S | ? | 0.02 | 0.04 | ||
3-葡糖苷酸雌三醇 | E2-3G | ? | 0.02 | 0.09 | ||
17β-葡糖苷酸雌三醇 | E2-17G | ? | 0.002 | 0.0002 | ||
苯甲酸雌二醇 | EB、3-苯甲酸雌二醇 | 10 | 1.1 | 0.52 | ||
17β-乙酸雌二醇 | E2-17A | 31–45 | 24 | ? | ||
二乙酸雌二醇 | EDA、3,17β-二乙酸雌二醇 | ? | 0.79 | ? | ||
丙酸雌二醇 | EP、17β-丙酸雌二醇 | 19–26 | 2.6 | ? | ||
戊酸雌二醇 | EV、17β-戊酸雌二醇 | 2–11 | 0.04–21 | ? | ||
環戊丙酸雌二醇 | EC、17β-環戊丙酸雌二醇 | ?c | 4.0 | ? | ||
棕櫚酸雌二醇 | 17β-棕櫚酸雌二醇 | 0 | ? | ? | ||
硬脂酸雌二醇 | 17β-硬脂酸雌二醇 | 0 | ? | ? | ||
雌酮 | E1、17-酮雌二醇 | 11 | 5.3–38 | 14 | ||
硫酸雌酮 | E1S、3-硫酸雌酮 | 2 | 0.004 | 0.002 | ||
葡糖苷酸雌酮 | E1G、3-葡糖苷酸雌酮 | ? | <0.001 | 0.0006 | ||
乙炔雌二醇 | EE、17α-乙炔雌二醇 | 100 | 17–150 | 129 | ||
美雌醇 | EE 3-甲醚 | 1 | 1.3–8.2 | 0.16 | ||
炔雌醚 | EE 3-環戊醚 | ? | 0.37 | ? | ||
腳本: a = 相對結合親和力(RBA)是通過標記的雌二醇從齧齒動物子宮胞質溶膠的雌激素受體(ER)的體外置換來確定的。在這些系統中,雌激素酯會不同程度地水解成雌激素(較短的酯鏈長度 -> 較高的水解速率),並且當水解被阻止時,酯的ER RBA會大大降低。[1][2] c = 环戊丙酸雌二醇对ER的亲和力与戊酸雌二醇和苯甲酸雌二醇相似 (数据).[4] Sources: 亲和力: [1][2][5][6][7] 雌激素效价强度: [8][9][10][11] 额外的: [4][3][12] |
模板文件
參見
參考資料
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