Wade G N, Heller H W
Department of Psychology, University of Massachusetts, Amherst 01003.
Am J Physiol. 1993 Jun;264(6 Pt 2):R1219-23. doi: 10.1152/ajpregu.1993.264.6.R1219.
Treatment of ovariectomized rats with the nonsteroidal antiestrogen tamoxifen mimicked the effects of estradiol and caused significant decreases in food intake and body weight. The decreases in body weight were reflected mainly in a decreased body fat content, although tamoxifen treatment did suppress linear growth too. Similar to the effects of estradiol, tamoxifen decreased parametrial white adipose tissue wet weight and lipoprotein lipase activity. When given concurrently with estradiol, tamoxifen showed no evidence of antiestrogenic activity on any of these measures. As reported previously, tamoxifen acted as a partial agonist/antagonist for uterine weight. The effective dose of tamoxifen for suppression of food intake, body weight, and body fat content fell between 10 and 50 micrograms/day. Therefore, tamoxifen behaves like other nonsteroidal antiestrogens and mimics but fails to antagonize the actions of estradiol on many aspects of physiological and behavioral regulation of energy balance.
用非甾体类抗雌激素他莫昔芬治疗去卵巢大鼠，可模拟雌二醇的作用，导致食物摄入量和体重显著下降。体重下降主要反映在体脂含量降低，不过他莫昔芬治疗也确实抑制了线性生长。与雌二醇的作用类似，他莫昔芬降低了子宫旁白色脂肪组织的湿重和脂蛋白脂肪酶活性。当与雌二醇同时给药时，他莫昔芬在这些指标上均未显示出抗雌激素活性。如先前报道，他莫昔芬对子宫重量起部分激动剂/拮抗剂的作用。他莫昔芬抑制食物摄入、体重和体脂含量的有效剂量在每日10至50微克之间。因此，他莫昔芬的行为与其他非甾体类抗雌激素相似，可模拟但无法拮抗雌二醇在能量平衡的生理和行为调节诸多方面的作用。
