Jarry Hubertus
Horm Mol Biol Clin Investig. 2013 Dec;16(1):7-12. doi: 10.1515/hmbci-2013-0034.
Abstract In the human female, menopause is the permanent end of fertility, defined as occurring 12 months after the last menstrual period. During peri- and postmenopausal stages, the vast majority of women experience moderate-to-severe vasomotor symptoms, such as hot flashes and night sweats, which interfere with sleep and may be severe enough to affect quality of life. The only treatment approved by national health authorities is hormone therapy with estrogen alone or in combination with a progestagen. However, this therapeutic regimen is associated with severe side effects, such as stimulation of growth of breast cancer or cardiovascular events. Thus, there is a demand for efficient and safe alternative treatments for menopausal complaints. After the discovery of estrogen receptor beta in many organs, and confirmation of its presence in the brain, many researchers raised the question of whether ERβ-specific ligands may be novel therapeutic agents for treatment of menopausal complaints with the desirable effects of estrogen but without increased risk of tumor incidence. This minireview will briefly summarize the relevance of estrogen receptor beta and its specific ligands for the treatment of menopausal symptoms with a focus on vasomotor menopausal symptoms. At present, estrogen receptor beta-selective ligands do not seem to be active in models of prevention or reversal of osteoporosis. However, data from animal experiments suggest that estrogen receptor beta-selective ligands might be safe therapeutics for the treatment of vasomotor menopausal symptoms.
摘要 在人类女性中，绝经是生育能力的永久终止，定义为末次月经后12个月。在围绝经期和绝经后阶段，绝大多数女性会经历中度至重度血管舒缩症状，如潮热和盗汗，这些症状会干扰睡眠，严重时可能影响生活质量。国家卫生当局批准的唯一治疗方法是单独使用雌激素或与孕激素联合使用的激素疗法。然而，这种治疗方案会带来严重的副作用，如刺激乳腺癌生长或引发心血管事件。因此，人们需要高效且安全的替代疗法来治疗绝经相关症状。在许多器官中发现雌激素受体β并证实其存在于大脑后，许多研究人员提出疑问，即雌激素受体β特异性配体是否可能成为治疗绝经相关症状的新型治疗药物，既能产生雌激素的理想效果，又不会增加肿瘤发生风险。本综述将简要总结雌激素受体β及其特异性配体在治疗绝经症状方面的相关性，重点关注血管舒缩性绝经症状。目前，雌激素受体β选择性配体在预防或逆转骨质疏松症的模型中似乎没有活性。然而，动物实验数据表明，雌激素受体β选择性配体可能是治疗血管舒缩性绝经症状的安全疗法。
