Selection and early clinical evaluation of the brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor UE2343 (Xanamem™)
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- 作者：Scott P Webster ; Andrew McBride ; Margaret Binnie ; Karen Sooy ; Jonathan R Seckl ; Ruth Andrew ; T David Pallin ; Hazel J Hunt ; Trevor R Perrior ; Vincent S Ruffles ; J William Ketelbey ; Alan Boyd and Brian R Walker
- 刊名：British Journal of Pharmacology
- 出版年：2017
- 出版时间：March 2017
- 年：2017
- 卷：174
- 期：5
- 页码：396-408
- 全文大小：1798K
- ISSN：1476-5381
文摘
Reducing glucocorticoid exposure in the brain via intracellular inhibition of the cortisol-regenerating enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) has emerged as a therapeutic strategy to treat cognitive impairment in early Alzheimer's disease (AD). We sought to discover novel, brain-penetrant 11β-HSD1 inhibitors as potential medicines for the treatment of AD.