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从艾氏海绵中分离出的一类C11N5化合物的抗毒蕈碱活性。

Anti-muscarinic activity of a family of C11N5 compounds isolated from Agelas sponges.

作者信息

Rosa R, Silva W, Escalona de Motta G, Rodríguez A D, Morales J J, Ortiz M

机构信息

Department of Chemistry, University of Puerto Rico, San Juan.

出版信息

Experientia. 1992 Sep 15;48(9):885-7. doi: 10.1007/BF02118426.

Abstract

In a search for potential target sites for C11N5 compounds obtained from marine sponges of the genus Agelas we evaluated their interaction with muscarinic acetylcholine receptors from rat brain membranes. In competition experiments with 3H-QNB these compounds displayed the following rank order of potency: sceptrin greater than oroidin greater than or equal to dibromosceptrin greater than or equal to clathrodin. Sceptrin (50 microM) was shown to be a competitive inhibitor of 3H-QNB binding as revealed by Scatchard analysis. The results demonstrate the ability of these compounds to interact with multiple target molecules in the micromolar range.

摘要

在寻找从阿盖拉属海洋海绵中获得的C11N5化合物的潜在靶点时,我们评估了它们与大鼠脑膜毒蕈碱型乙酰胆碱受体的相互作用。在与3H-QNB的竞争实验中,这些化合物表现出以下效力顺序:sceptrin>oroidin≥二溴sceptrin≥clathrodin。Scatchard分析表明,sceptrin(50μM)是3H-QNB结合的竞争性抑制剂。结果证明了这些化合物在微摩尔范围内与多种靶分子相互作用的能力。

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