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Further lead optimization efforts on previously described 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles led to the new class of 5,5a,6,7,8,9-hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines culminating in the discovery of (5aR,9R)-2-[(cyclopropylmethoxy)methyl]-5,5a,6,7,8,9-hexahydro-9-methyl-pyrido[3', 2':4,5]pyrrolo[1,2-a]pyrazine 18 as a potent, full 5-HT(2C) receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.

Original publication

DOI

10.1016/j.bmcl.2005.11.083

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/03/2006

Volume

16

Pages

1207 - 1211

Keywords

Animals, CHO Cells, Cricetinae, Humans, Hydroxylation, Molecular Structure, Phospholipids, Pyrazines, Pyrroles, Receptor, Serotonin, 5-HT2C, Serotonin 5-HT2 Receptor Agonists, Structure-Activity Relationship