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Bioorg Med Chem Lett. 2006 Aug 1;16(15):4130-4. Epub 2006 Jun 5.

The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.

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

Abstract

5-HT2C agonists have shown efficacy in limiting food consumption and thus may serve as an important drug class in combating obesity. We describe the design and synthesis of a novel tricyclic single-nitrogen scaffold that was used to produce 5-HT2C agonists. SAR was developed around this chemotype and compounds were identified that were potent (Ki<15 nM) and selective relative to other 5-HT2 receptors. The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats.

PMID:
16750364
DOI:
10.1016/j.bmcl.2006.04.070
[Indexed for MEDLINE]
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