Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Röver S., Adams DR., Bénardeau A., Bentley JM., Bickerdike MJ., Bourson A., Cliffe IA., Coassolo P., Davidson JEP., Dourish CT., Hebeisen P., Kennett GA., Knight AR., Malcolm CS., Mattei P., Misra A., Mizrahi J., Muller M., Porter RHP., Richter H., Taylor S., Vickers SP.
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.