Baudendistel L J, Ruh M F, Nadel E M, Ruh T S
Acta Endocrinol (Copenh). 1978 Nov;89(3):599-611. doi: 10.1530/acta.0.0890599.
The effect of the in vivo administration of various triphenylethylene antioestrogens and physiological (0.05 microgram) versus pharmacological (0.5--5 microgram) doses of oestradiol-17 beta (Oe2) on the uterotrophic process in general and the nuclear accumulation and cytoplasmic depletion and replenishment of uterine oestrogen receptor was determined. Regardless of the dose of Oe2 the changes in uterine wet weight, total protein and incorporation of [3H]thymidine into DNA and [14C]leucine into protein were the same at 24 h. The anti-oestrogen receptor was also studied. The net increase, above control, of cytoplasmic oestrogen receptor at 24 h and 48 h after Oe2 injection was approximately 0.35 and 0.77 pmoles/uterus, respectively. The effect of anti-oestrogens (U-11,100A, CI628, en- and zuclomiphene) on the increase in cytoplasmic oestrogen receptor at 24 h and 48 h measured from maximally depleted levels was nearly identical to the Oe2 induced net increase. This suggests that in both cases these particular increases represent newly synthesized receptor and that Oe2 causes some receptor replenishment through a recycling process.
测定了各种三苯乙烯类抗雌激素药物的体内给药以及生理剂量(0.05微克)与药理剂量(0.5 - 5微克)的17β-雌二醇(Oe2)对子宫营养过程以及子宫雌激素受体的核积累、细胞质耗竭和补充的影响。无论Oe2的剂量如何,在24小时时子宫湿重、总蛋白以及[3H]胸腺嘧啶掺入DNA和[14C]亮氨酸掺入蛋白质的变化都是相同的。还研究了抗雌激素受体。Oe2注射后24小时和48小时,细胞质雌激素受体相对于对照的净增加量分别约为0.35和0.77皮摩尔/子宫。从最大耗竭水平测量,抗雌激素(U - 11,100A、CI628、恩氯米芬和左氯米芬)对24小时和48小时细胞质雌激素受体增加的影响与Oe2诱导的净增加几乎相同。这表明在这两种情况下,这些特定的增加代表新合成的受体,并且Oe2通过再循环过程导致一些受体补充。