Brasili L, Angeli P, Brancia E, Melchiorre C
Eur J Pharmacol. 1984 Aug 3;103(1-2):181-4. doi: 10.1016/0014-2999(84)90209-7.
In an attempt to further improve the alpha-adrenoreceptor blocking activity of benextramine, the effect of heteroaromatic substituents on the terminal nitrogens was studied. In this communication we report on the newly synthetized N,N''-(dithio-2,1-ethanediyl)bis[N'-(pyrrol-2-ylmethyl)-1,6- hexanediamine] (pyrextramine) that displayed higher affinity (5-10-fold) and higher selectivity (about 12-fold) than benextramine. These preliminary results show that pyrextramine can replace benextramine in the elucidation and characterization of the peripheral alpha 1-adrenoreceptors.
为了进一步提高苄环烷的α-肾上腺素能受体阻断活性，研究了在末端氮原子上引入杂芳基取代基的效果。在本通讯中，我们报道了新合成的N,N''-(二硫代-2,1-亚乙基)双N'-(吡咯-2-基甲基)-1,6-己二胺，它比苄环烷表现出更高的亲和力(5-10倍)和更高的选择性(约12倍)。这些初步结果表明，吡咯苄胺可在对外周α1-肾上腺素能受体的阐释和表征中取代苄环烷。
