title: Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.
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.
authors: Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.
authors: David R
authors: DR
authors: Bauman
authors: Alan
authors: A
authors: Whitehead
authors: Lisa C
authors: LC
authors: Contino
authors: Jisong
authors: J
authors: Cui
authors: Margarita
authors: M
authors: Garcia-Calvo
authors: Xin
authors: X
authors: Gu
authors: Nancy
authors: N
authors: Kevin
authors: Xiuying
authors: X
authors: Ma
authors: Lee-yuh
authors: LY
authors: Pai
authors: Kashmira
authors: K
authors: Shah
authors: Xiaolan
authors: X
authors: Shen
authors: Sloan
authors: S
authors: Stribling
authors: Hratch J
authors: HJ
authors: Zokian
authors: Joe
authors: J
authors: Metzger
authors: Diane E
authors: DE
authors: Shevell
authors: Sherman T
authors: ST
authors: Waddell
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000201:enzymology*; D051379:Mice; D018345:Mice, Knockout; D051381:Rats; D011918:Rats, Inbred SHR; D014230:Triazoles / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D014230:Triazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1