Miseková D, Lincová D, Mühlbachová E
Department of Pharmacology, Faculty of Medicine, Charles University, Prague.
Physiol Bohemoslov. 1989;38(2):145-53.
The authors studied changes in adrenergic lipolysis in the epididymal adipose tissue of rats to which diethylstilboestrol and oestradiol combined with the anti-oestrogen clomiphene were administered. The maximum lipid-mobilizing effect of isoprenaline was increased not only by subcutaneously administered diethylstilboestrol, but also by the highest dose of the antioestrogen clomiphene used (p.o., 200 micrograms.kg-1 b.w.). Under the given experimental conditions, with 4 1/2 h incubation of adipose tissue, clomiphene was also effective when added in vitro. Its own oestrogenic effect probably stimulated the lipid-mobilizing action of isoprenaline. On combining the administration of increasing doses of clomiphene (p.o., 1-5 days) with a constant dose of oestradiol (200 micrograms.kg-1, s.c. on the 8th day, i.e. 24 h before the actual experiment), changes in isoprenaline lipolysis depended on the dose of clomiphene. In low doses clomiphene inhibited the stimulating effect of subsequently administered oestradiol on isoprenaline-induced lipolysis, but in large doses (100 and 200 micrograms.kg-1 daily) it potentiated, together with oestradiol, the lipid-mobilizing effect of isoprenaline. The results show that the non-steroid oestrogen diethylstilboestrol and the antioestrogen clomiphene may be included among the hormones capable of altering the response of adipose tissue to sympathomimetics (isoprenaline). We attribute the fact that clomiphene acted either as an antagonist or as an agonist of oestradiol to its combined oestrogenic and anti-oestrogenic effects.
作者研究了给大鼠附睾脂肪组织注射己烯雌酚、雌二醇以及与抗雌激素克罗米酚联合使用时，肾上腺素能脂解作用的变化。皮下注射己烯雌酚以及使用最高剂量（口服，200微克·千克⁻¹体重）的抗雌激素克罗米酚均可增强异丙肾上腺素的最大脂解作用。在给定的实验条件下，脂肪组织孵育4.5小时，克罗米酚体外添加时也有效果。其自身的雌激素效应可能刺激了异丙肾上腺素的脂解作用。将递增剂量的克罗米酚（口服，1 - 5天）与恒定剂量的雌二醇（200微克·千克⁻¹，第8天皮下注射，即实际实验前24小时）联合使用时，异丙肾上腺素脂解作用的变化取决于克罗米酚的剂量。低剂量时，克罗米酚抑制随后给予的雌二醇对异丙肾上腺素诱导脂解的刺激作用，但高剂量（每日100和200微克·千克⁻¹）时，它与雌二醇一起增强了异丙肾上腺素的脂解作用。结果表明，非甾体雌激素己烯雌酚和抗雌激素克罗米酚可被列入能够改变脂肪组织对拟交感神经药（异丙肾上腺素）反应的激素之中。我们将克罗米酚对雌二醇表现为拮抗剂或激动剂的事实归因于其兼具的雌激素和抗雌激素作用。
