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Farmasøytiske preparater for mÕlrettet erstatning av østrogenmangel i sentralnervesystemet

机译:靶向治疗中枢神经系统雌激素缺乏症的药物制剂

摘要

Selected steroids are used to produce pharmaceutical preparations for selectively supplementing oestrogen deficiency in the central nervous system (CNS) without influencing other organs or systems. These steroids are characterised in that they have a selective, neurotropic, oestrogen-like transcription effect, unlike the systemically active natural and synthetic oestrogens, including 17a-estradiol. It has been surprisingly discovered that the selected steroids, when used according to the invention, selectively influence the transcription of oestrogen-dependent genes in the central nervous system and cause alterations of the corresponding physiological parameters; have transcription effects specific to the central nervous systems in doses which have no biological effects on the tissues of the reproductive system; have transcription effects specific to the central nervous system at doses at which neither 17b-estradiol nor 17a-estradiol have any effect; and do not influence the transcription of oestrogen-dependent genes in the central nervous system to a greater extent than the secondary 17b-estradiol.
机译:选定的类固醇用于生产药物制剂,以选择性补充中枢神经系统(CNS)中的雌激素缺乏症,而不会影响其他器官或系统。这些类固醇的特征在于它们具有选择性的,神经质的,类似于雌激素的转录作用,这与包括17a-雌二醇在内的具有系统活性的天然和合成雌激素不同。令人惊讶地发现,当根据本发明使用时,所选择的类固醇选择性地影响中枢神经系统中雌激素依赖性基因的转录,并引起相应生理参数的改变。具有对中枢神经系统特有的转录作用,其剂量对生殖系统的组织没有生物学影响;在17b-雌二醇和17a-雌二醇都不起作用的剂量下,具有中枢神经系统特有的转录作用;并且不会比次级17b-雌二醇更大程度地影响中枢神经系统中雌激素依赖性基因的转录。

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