硫代环庚吡啶嗪作为新的毒蕈碱剂。

Drug design and discovery Pub Date : 1997-04-01

D Barlocco, G Cignarella, F Fanelli, B Vitalis, P Matyus, P G De Benedetti

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引用次数: 0

摘要

合成了一系列与米那普利结构相关的噻吩环庚吡嗪类化合物(3aa-dd)，并对其与毒菌碱受体的亲和力进行了测试。它们对拮抗剂3H-QNB和激动剂3H-OXO-M的Ki值均在微摩尔范围内，表明它们对毒蕈碱受体起拮抗剂作用。此外，对他们的相互作用行为进行了理论研究与人类m1毒蕈碱受体的三维(3-D)模型。

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Thienocycloheptapyridazines as new muscarinic agents.

A series of thienocycloheptapyridazines (3aa-dd), structurally related to Minaprine, was synthesized and compounds tested for their affinity towards muscarinic receptors. All of them showed Ki values in the micromolar range towards both the antagonist 3H-QNB and the agonist 3H-OXO-M, thus indicating that they act as antagonists at the muscarinic receptors. Moreover a theoretical study was performed on their interaction behaviour with a three dimensional (3-D) model of the human m1 muscarinic receptor.

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Drug design and discovery

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