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Bioorg Med Chem Lett. 2005 Aug 1;15(15):3604-8.

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

Author information

1
Vernalis Research Ltd., Oakdene Court, 613 Reading Road, Wokingham RG41 5UA, UK. stephan.roever@roche.com

Abstract

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.

PMID:
15975787
DOI:
10.1016/j.bmcl.2005.05.074
[Indexed for MEDLINE]

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