1-芳基哌嗪基-4-环己胺衍生的异吲哚-1,3-二酮作为强效且选择性的α-1a/1d肾上腺素能受体配体。
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
作者信息
Li Shengjian, Chiu George, Pulito Virginia L, Liu Jingchun, Connolly Peter J, Middleton Steven A
机构信息
Johnson & Johnson Pharmaceutical Research and Development LLC, Drug Discovery Research, PO Box 300, 1000 Route 202 South, Raritan, NJ 08869, USA.
出版信息
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1646-50. doi: 10.1016/j.bmcl.2006.12.111. Epub 2007 Jan 12.
Subtype-selective alpha-1a and/or alpha-1d adrenergic receptor antagonists may be useful for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) with fewer adverse effects than non-selective drugs. A series of 1-arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones has been synthesized, displaying in vitro alpha(1a) and alpha(1d) binding affinity K(i) values in the range of 0.09-38nM with K(i)(alpha1b)/K(i)(alpha1a) and K(i)(alpha1b)/K(i)(alpha1d) selectivity ratios up to 3607-fold.
亚型选择性α-1a和/或α-1d肾上腺素能受体拮抗剂可能对治疗良性前列腺增生（BPH）和下尿路症状（LUTS）有用，且副作用比非选择性药物少。已经合成了一系列1-芳基哌嗪基-4-环己胺衍生的异吲哚-1,3-二酮，其在体外显示出α(1a)和α(1d)结合亲和力K(i)值在0.09 - 38nM范围内，K(i)(α1b)/K(i)(α1a)和K(i)(α1b)/K(i)(α1d)选择性比率高达3607倍。
Zotero 插件