Potential antisecretory antidiarrheals. 1. .alpha.2-Adrenergic aromatic aminoguanidine hydrazones
作者:Barnett S. Pitzele、Alan E. Moormann、Gary W. Gullikson、David Albin、Robert G. Bianchi、Prima Palicharla、Elizabeth L. Sanguinetti、D. Eric Walters
DOI:10.1021/jm00396a020
日期:1988.1
using a rabbit ileum preparation. A number of compounds, including members of each structural class, were active upon subcutaneous administration in the rat. Active compounds were determined to be alpha 2-adrenergic agonists by yohimbine reversals of their Ussing chamber activities. The compound displaying the best separation of activities was the aminoguanidine hydrazone of 2,6-dimethyl-4-hydroxybenzaldehyde
瓜纳本斯,一种中枢性降压药,已显示具有肠道抗分泌特性。为了分离抗分泌和心血管活性,制备了一系列芳香族氨基胍and。合成了苯甲醛,萘醛和四氢萘酮衍生物。使用兔回肠制剂,在霍乱毒素治疗的大鼠结扎空肠中和Ussing室中评估化合物。在大鼠皮下给药后,许多化合物(包括每个结构类别的成员)均具有活性。通过育亨宾逆转其Ussing室活动,确定活性化合物为α2-肾上腺素能激动剂。表现出最佳分离活性的化合物是2,6-二甲基-4-羟基苯甲醛的氨基胍(20)。