Schäfer G, Krause W
Arch Dermatol Res. 1985;277(3):230-4. doi: 10.1007/BF00404322.
To evaluate the antagonism between estradiol and tamoxifen in the sebaceous gland of the hamster ear, animals were topically treated, and the size of the sebaceous glands was measured by histoplanimetry. The systemic effects were described by determining the estradiol and testosterone plasma levels and within the testes, and the size of the seminal vesicles and the contralateral sebaceous gland. The administration of 0.1 micrograms estradiol resulted in a diminution in the size of the treated glands but left all other parameters unchanged, indicating a purely local effect. A higher dose of estradiol (1 microgram) further decreased the size of the treated glands, but this was combined with a systemic effect, i.e. low plasma testosterone, decrease in testis size and a diminution of the contralateral ear gland. Ten micrograms of estradiol maximally suppressed all of the androgen effects without side effects. The administration of tamoxifen alone also decreased the size of the sebaceous glands without side effects, but it did not affect the production or effects of androgens. When administered in combination with estradiol, it antagonized the effects of this hormone completely. We conclude that tamoxifen inhibits the negative effect of estradiol on sebaceous-gland size. It acts predominantly in a systemic manner, because a metabolisation to monohydroxytamoxifen is necessary.
为评估雌二醇与他莫昔芬在仓鼠耳部皮脂腺中的拮抗作用，对动物进行局部处理，并通过组织平面测量法测量皮脂腺大小。通过测定血浆雌二醇和睾酮水平以及睾丸、精囊和对侧皮脂腺的大小来描述全身效应。给予0.1微克雌二醇会导致处理过的腺体大小减小，但其他所有参数均未改变，表明这是一种纯粹的局部效应。更高剂量的雌二醇（1微克）进一步减小了处理过的腺体大小，但这伴随着全身效应，即血浆睾酮水平降低、睾丸大小减小以及对侧耳部腺体减小。10微克雌二醇最大程度地抑制了所有雄激素效应且无副作用。单独给予他莫昔芬也会减小皮脂腺大小且无副作用，但它不影响雄激素的产生或作用。当与雌二醇联合给药时，它完全拮抗了这种激素的作用。我们得出结论，他莫昔芬抑制雌二醇对皮脂腺大小的负面影响。它主要以全身方式起作用，因为需要将其代谢为单羟基他莫昔芬。
