Heteroadamantyl Cannabinoids
Heteroadamantyl Cannabinoids
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DOI：
10.1021/jm100390h
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发表时间：
2010-08-12
影响因子：
7.3
通讯作者：
Makriyannis, Alexandros
中科院分区：
文献类型：
--
作者：
Dixon, Darryl D.;Sethumadhavan, Divakaramenon;Makriyannis, Alexandros
脂肪族侧链在决定三环经典大麻素的大麻能效力中起着关键作用。我们已经合成了一系列类似物，其中C3位置被金刚烷胺或氧杂或氧氮杂金刚烷直接或通过一个碳原子连接体取代。类似物16中的氧杂金刚烷药效团显示出对两种受体的最佳结合特征。
The aliphatic side chain plays a pivotal role in determining the cannabinergic potency of tricyclic classical cannabinoids. We have synthesized a series of analogues in which the C3 position is substituted either directly or through a one-carbon atom linker with an adamantylamine or with an oxa- or an oxazaadamantane. The oxaadamantane pharmacophore in analogue 16 showed the best binding profile for both receptors.