Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2

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36

摘要:

The preparation of a number of (bis)guanidine and (bis)2-aminoimidazoline derivatives as potential α 2 -adrenoceptor antagonists for the treatment of depression is presented. Human brain tissue was used to measure their affinity toward the α 2 -adrenoceptors in vitro. Compounds 6b , 8b , 9b , 10b , 15b , 17b , 18b , 20b , and 21b displayed a good affinity (p K i > 7) and were evaluated in in vitro functional [ 35 S]GTPγS binding assays in human prefrontal cortex to determine their agonistic or antagonistic activity. Among these compounds, 17b and 20b showed the expected behavior for an antagonist and were subject to in vivo microdialysis experiments in rats. Significantly, these experiments confirmed the antagonistic properties of 17b and 20b , and therefore both compounds can be considered as potential antidepressants.

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DOI:

10.1021/jm800026x

被引量:

58

年份:

2008

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来源期刊

J.med.chem
May 7, 2008

引用走势

2009
被引量:11

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