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Bioorg Med Chem Lett. 2006 Jun 1;16(11):2891-4. Epub 2006 Mar 20.

The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists.

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1
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. brhuck@hotmail.com

Abstract

The 5-HT2C receptor has been implicated in the regulation of appetite. As such, small molecule agonists to this receptor may serve as novel therapies to combat obesity. We describe here the identification, synthesis, and SAR of a 5-HT2C agonist from a unique pyrimidine-diazabicyclo[3.3.0]octane series. This compound displayed good potency at the 5-HT2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats.

PMID:
16546379
DOI:
10.1016/j.bmcl.2006.03.007
[Indexed for MEDLINE]
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