DESIGN, SYNTHESIS AND PHARMACOLOGY OF CANNABIMIMETIC INDOLES
DESIGN, SYNTHESIS AND PHARMACOLOGY OF CANNABIMIMETIC INDOLES
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DOI：
10.1016/s0960-894x(01)80155-4
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发表时间：
1994-02-24
影响因子：
2.7
通讯作者：
COMPTON, DR
中科院分区：
文献类型：
--
作者：
HUFFMAN, JW;DAI, D;COMPTON, DR
采用分子模型设计了一组新的大麻模拟1-烷基-2-甲基-3-（1-萘基）吲哚。通过测定与大麻素受体的结合，在小鼠体内和体外评估大麻素活性。1-丁基、戊基和己基类似物活性最大。提出了这些吲哚与传统大麻素对齐的合理化
Molecular modeling has been employed to design a new group of cannabimimetic 1-alkyl-2-methyl-3-(1-naphthoyl)indoles. Cannabinoid activity was evaluated in vivo in the mouse and in vitro by determining the binding to the cannabinoid receptor. Maximum activity was found for the 1-butyl, pentyl and hexyl analogs. A rationalization for the alignment of these indoles with traditional cannabinoids is presented