Synthesis, pharmacology and therapeutic potential of 10-methoxypyrazino[1,2-a]indoles, partial agonists at the 5HT(2C) receptor
Synthesis, pharmacology and therapeutic potential of 10-methoxypyrazino[1,2-a]indoles, partial agonists at the 5HT(2C) receptor
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DOI：
10.1016/s0223-5234(97)83976-1
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发表时间：
1997-01-01
影响因子：
6.7
通讯作者：
Widmer, U
中科院分区：
文献类型：
--
作者：
Bos, M;Jenck, F;Widmer, U
制备了一系列新的10-甲氧基吡嗪[1,2- A]吲哚，并证明它们是5HT（2C）受体配体。所研究的化合物10a-j被发现在5HT（2C）受体上作为部分激动剂，与5HT（1A）和5HT（2A）受体结合具有高亲和力和中等选择性，但仅诱导磷酸肌醇形成的次极大增加。化合物10j在强迫症、抑郁症和惊恐焦虑动物模型中均有活性。
A series of new 10-methoxypyrazino[1,2-a]indoles has been prepared and shown to be 5HT(2C) receptor ligands. The studied compounds 10a-j were found to act as partial agonists at the 5HT(2C) receptor, binding with high affinity and moderate selectivity versus 5HT(1A) and 5HT(2A) receptors, but inducing only a submaximal increase in phosphoinositol formation. Compound 10j was demonstrated to be active in animal models of obsessive-compulsive disorder, depression and panic anxiety.