SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME 1,2,3-TRIAZOLE DERIVATIVES
SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME 1,2,3-TRIAZOLE DERIVATIVES
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DOI：
10.1002/jps.2600771117
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发表时间：
1988-11-01
影响因子：
3.8
通讯作者：
LIVI, O
中科院分区：
文献类型：
--
作者：
MARTINI, C;MARRUCCI, W;LIVI, O
制备了一些1，2，3-三氮唑类化合物，并测试了它们从牛脑组织膜上置换[~3H]地西潘的能力。从这些化合物中，喹啉基三氮唑衍生物(14，15，16，17)显然是最有效的，而萘基和萘甲基三氮唑的活性要低得多。对硝基苯衍生物(15)是喹啉基三氮唑类化合物中结合亲和力最高的化合物。对硝基苯基被其他取代基取代后，结合活性大大降低。从Lineweaver-Burk对11的分析中，似乎这种抑制是竞争性的。
Certain 1,2,3‐triazole derivatives were prepared and tested for their ability to displace [3H]diazepam from bovine brain membranes. From these compounds, the quinolyltriazole derivatives (14,15,16,17) were clearly the most potent, while the naphthyl‐ and the naphthyridyltriazoles were considerably less active. Thep‐nitrophenyl derivative (15) was the compound that bound with the highest affinity within the quinolyltriazole compounds class. The replacement of thep‐nitrophenyl group with other substituents greatly decreased the binding activity. From a Lineweaver‐Burk analysis of11, it appears that the inhibition is competitive.