选择性雌激素受体调节剂：组织作用及中枢神经系统保护潜力
Selective estrogen receptor modulators: tissue actions and potential for CNS protection.
作者信息
Littleton-Kearney M T, Ostrowski N L, Cox D A, Rossberg M I, Hurn P D
机构信息
Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA.
出版信息
CNS Drug Rev. 2002 Fall;8(3):309-30. doi: 10.1111/j.1527-3458.2002.tb00230.x.
Abstract
Significant physiologic changes occur during menopause. Evidence exists to suggest that estrogen may be neuroprotective under specific conditions. However, there are limitations in the neuroprotection afforded by standard hormone therapy. Accordingly, alternative agents with selected estrogenic effects may hold even greater promise rather than conventional hormone replacement therapy for the prevention and treatment of CNS injury. Recently, a variety of selective estrogen receptor modulators (SERMs) have been developed to retain the favorable and minimize the adverse side effects of estrogens. This review focuses on the CNS and known neuroprotective effects of two specific SERMs, raloxifene and arzoxifene. Recent studies hint that raloxifene and arzoxifene are neuroprotective and may preserve some elements of cognitive function. However, the mechanism of action is not well described and it is unclear if the beneficial effects of SERMs rely on activation of estrogen receptors.
摘要
更年期会发生显著的生理变化。有证据表明，雌激素在特定条件下可能具有神经保护作用。然而，标准激素疗法所提供的神经保护存在局限性。因此，具有特定雌激素效应的替代药物对于中枢神经系统损伤的预防和治疗可能比传统激素替代疗法更具前景。最近，已开发出多种选择性雌激素受体调节剂（SERM），以保留雌激素的有益作用并将其不良副作用降至最低。本综述重点关注两种特定SERM（雷洛昔芬和阿佐昔芬）对中枢神经系统的作用及已知的神经保护作用。最近的研究表明，雷洛昔芬和阿佐昔芬具有神经保护作用，可能会保留一些认知功能要素。然而，其作用机制尚未得到充分描述，且SERM的有益效果是否依赖于雌激素受体的激活尚不清楚。
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