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  3. Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension

Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension

  • Bioorg Med Chem Lett. 2013 Jun 15;23(12):3650-3. doi: 10.1016/j.bmcl.2013.03.011.
David R Bauman 1,  Alan Whitehead,  Lisa C Contino,  Jisong Cui,  Margarita Garcia-Calvo,  Xin Gu,  Nancy Kevin,  Xiuying Ma,  Lee-yuh Pai,  Kashmira Shah,  Xiaolan Shen,  Sloan Stribling,  Hratch J Zokian,  Joe Metzger,  Diane E Shevell,  Sherman T Waddell
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.
PMID: 23659858 DOI: 10.1016/j.bmcl.2013.03.011
Abstract

In an effort to understand the origin of blood-pressure lowering effects observed in recent clinical trials with 11β-HSD1 inhibitors, we examined a set of 11β-HSD1 inhibitors in a series of relevant in vitro and in vivo assays. Select 11β-HSD1 inhibitors reduced blood pressure in our preclinical models but most or all of the blood pressure lowering may be mediated by a 11β-HSD1 independent pathway.

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