Synthesis, characterization and pharmacological profile of tropicamide enantiomers

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• 作者：Dei ; Silvia ; Bellucci ; Cristina ; Romanelli ; M. Novella ; Ghelardini ; Carla ; Spampinato ; Santi
• 关键词：tropicamide enantiomers ; M₄ selective muscarinic antagonist ; M₁-M₄ subtypes ; analgesia
• 刊名：Life Sciences
• 出版年：1996
• 期刊代码：62_00243205
• 类别：imm
• 出版时间：May 3, 1996
• 卷：58
• 期：23
• 页码：2147-2153
• 文件大小：435 K

摘要

The synthesis, chemical characterization and antimuscarinic activity of the two enantiomers of tropicamide are reported. Functional (rabbit vas deferens, guinea pig heart (force) and ileum) as well as binding experiments (m₁ and m₄ human muscarinic receptors expressed in CHO-K1 cells; M₂ and M₃ receptors of rat heart and submaxillary gland membranes) were used to evaluate the antimuscarinic activity of the enantiomers. The results show that none of the enantiomers is able to significantly discriminate among the receptors studied and therefore do not support the proposal of tropicamide as an M₄ (m₄) selective agent.