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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.

Original publication

DOI

10.1016/j.bmcl.2005.05.074

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/08/2005

Volume

15

Pages

3604 - 3608

Keywords

Animals, Eating, Indoles, Injections, Subcutaneous, Pyrazines, Pyridines, Rats, Rats, Wistar, Serotonin 5-HT2 Receptor Agonists, Serotonin Receptor Agonists, Structure-Activity Relationship