β₃-Adrenoceptor agonists for the treatment of frequent urination and urinary incontinence: 2-[4-(2-{[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino}ethyl)pheno

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• 作者：Tanaka ; Nobuyuki ; Tamai ; Tetsuro ; Mukaiyama ; Harunobu ; Hirabayashi ; Akihito ; Muranaka ; Hideyuki ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2001
• 出版时间：December, 2001
• 年：2001
• 卷：9
• 期：1
• 页码：3265-3271
• 全文大小：174 K

文摘

In a search for novel analogues of β₃-adrenoceptor (AR) agonists relaxing the bladder for treatment of urinary dysfunction, 2-[4-(2-{[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino}ethyl)phenoxy]-2-methylpropionic acids (1a–e), into which a fibrate-like structure had been incorporated, were synthesised. Compound 1a was found to be a selective β₃-AR agonist in functional assays using the ferret detrusor (β₃-AR), rat uterus (β₂-AR), and rat atrium (β₁-AR); β₃: EC₅₀