| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367974 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
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.
Graphical abstractNew 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 full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists](/preview/png/1367974.png "First Page Preview: Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists")
Authors
S. Röver, D.R. Adams, A. Bénardeau, J.M. Bentley, M.J. Bickerdike, A. Bourson, I.A. Cliffe, P. Coassolo, J.E.P. Davidson, C.T. Dourish, P. Hebeisen, G.A. Kennett, A.R. Knight, C.S. Malcolm, P. Mattei, A. Misra, J. Mizrahi, M. Muller, R.H.P. Porter,