鉴定4-甲基-1,2,3,4,10,10a-六氢吡嗪并[1,2-a]吲哚为5-HT2C受体激动剂。
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
作者信息
Röver S, Adams D R, Bénardeau A, Bentley J M, Bickerdike M J, Bourson A, Cliffe I A, Coassolo P, Davidson J E P, Dourish C T, Hebeisen P, Kennett G A, Knight A R, Malcolm C S, Mattei P, Misra A, Mizrahi J, Muller M, Porter R H P, Richter H, Taylor S, Vickers S P
机构信息
Vernalis Research Ltd., Oakdene Court, 613 Reading Road, Wokingham RG41 5UA, UK.
出版信息
Bioorg Med Chem Lett. 2005 Aug 1;15(15):3604-8. doi: 10.1016/j.bmcl.2005.05.074.
Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists.
描述了新型4-甲基-1,2,3,4,10,10a-六氢吡嗪并[1,2-a]吲哚作为5-HT(2C)受体激动剂的合成及其活性评估。经过适当取代后，几种类似物对其他5-HT(2)受体亚型表现出1个数量级或更高的选择性。与先导化合物1相比，几种化合物的选择性得到了提高，增加了对这一系列5-HT(2C)受体激动剂的治疗兴趣。
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