Collins D C, Balikian H M, Robinson H R, Preedy J R
Am J Physiol. 1979 Apr;236(4):E347-57. doi: 10.1152/ajpendo.1979.236.4.E347.
The effect of the drug sulfobromophthalein (BSP) on plasma estrogens in the dog were studied during intravenous infusions of 3H-labeled estrogens. During [3H]estrone infusion, BSP administration caused a marked increase in arterial plasma levels of the radioactive conjugated estrogens, estrone glucosiduronate, estradiol-17 beta glucosiduronate(s), and estrone sulfate. Levels of the unconjugated estrogens, estrone and estradiol-17 beta, were substantially unaltered. Possible mechanisms were investigated. Splanchnic extraction of the conjugates did not change significantly during BSP administration, and renal excretion rose promptly in proportion to the plasma levels, thus virtually excluding decreased biliary or renal excretion. There was no net discharge of estrogen glucosiduronate radioactivity from adipose tissue or muscle following BSP. During [3H]estrone glucosiduronate infusion, BSP again caused an increase in plasma estrone glucosiduronate, thus excluding increased formation (of this conjugate, at least). BSP caused decreased extraction of estrone glucosiduronate by the hindlimb, indicating that decreased metabolism was the probable cause of the elevated plasma levels. BSP also caused decreased formation of unconjugated estrogens by the lungs, indicating that the decreased metabolism includes decreased hydrolysis of estrogen glucosiduronates.
在静脉输注3H标记的雌激素期间，研究了药物磺溴酞钠（BSP）对犬血浆雌激素的影响。在输注[3H]雌酮期间，给予BSP导致动脉血浆中放射性结合雌激素、雌酮葡萄糖醛酸酯、雌二醇-17β葡萄糖醛酸酯和硫酸雌酮的水平显著升高。未结合雌激素雌酮和雌二醇-17β的水平基本未改变。对可能的机制进行了研究。在给予BSP期间，结合物的内脏提取没有显著变化，并且肾脏排泄与血浆水平成比例迅速增加，因此实际上排除了胆汁或肾脏排泄减少的情况。给予BSP后，脂肪组织或肌肉中没有雌激素葡萄糖醛酸酯放射性的净释放。在输注[3H]雌酮葡萄糖醛酸酯期间，BSP再次导致血浆雌酮葡萄糖醛酸酯增加，因此至少排除了（这种结合物）形成增加的情况。BSP导致后肢对雌酮葡萄糖醛酸酯的提取减少，表明代谢减少可能是血浆水平升高的原因。BSP还导致肺中未结合雌激素的形成减少，表明代谢减少包括雌激素葡萄糖醛酸酯水解减少。
