申请人:Stamler S. Jonathan
公开号:US20070258942A1
公开(公告)日:2007-11-08
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without ghitathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.
一种分子量范围为225至1,000(口服为225至600)的C-亚硝基化合物,其基础单体中亚硝基基团连接到三级碳上,通过对pKa小于约25的碳酸的亚硝基化获得,可用作NO供体。当该化合物由pKa小于约10的碳酸获得时,在微摩尔浓度下使用可提供血管松弛作用,且该活性在谷胱甘肽的作用下可在纳摩尔浓度下获得。当该化合物由pKa约为15至20的碳酸获得时,可在纳摩尔浓度下获得血管松弛作用而无需谷胱甘肽。在另一实施例中,一种生物相容性聚合物包含C-亚硝基基团。