Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT2 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-HT2C receptor agonists.

New 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles are 5-HT2C receptor agonists. Appropriately substituted, several analogs show high potency and appreciable selectivity against the other 5-HT2 receptor subtypes.Figure optionsDownload as PowerPoint slide