Soft drugs. 3. A new class of anticholinergic agents
作者:Nicholas Bodor、Ross Woods、Colin Raper、Pauline Kearney、James J. Kaminski
DOI:10.1021/jm00179a002
日期:1980.5
hindered "umbrella" acids and cholinergics when derivatives of simple aliphatic acids. The more potent anticholinergics have up to 10 times higher acetylcholine antagonist activity than atropine, but they have a much shorter duration of action. The compounds cleave hydrolytically with simultaneous destruction of the quaternary head. The compounds are promising as selective, local agents, particularly as
设计并合成了一类新的抗毒蕈碱药物。这些化合物是“软”季铵酯,其中只有一个碳原子将酯氧和季头分开。当衍生自受阻的“伞”酸时,该化合物是有效的抗胆碱能药,而当衍生自简单脂肪酸时,这些化合物是胆碱能药。与阿托品相比,更有效的抗胆碱能药具有高达10倍的乙酰胆碱拮抗剂活性,但作用时间却短得多。该化合物水解裂解,同时破坏四级头。该化合物有望作为选择性的局部药物,特别是作为内分泌出汗的抑制剂。