|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
15
|
|
pubmed:dateCreated |
2006-6-20
|
|
pubmed:abstractText |
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.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Aug
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BennaniYoussef LYL,
pubmed-author:BrundenKurt RKR,
pubmed-author:CrumrineChrisC,
pubmed-author:DentThomas CTC,
pubmed-author:HarringtonJohnJ,
pubmed-author:HodnickWilliam FWF,
pubmed-author:HuckBayard RBR,
pubmed-author:LlamasLuisL,
pubmed-author:RobargeMichael JMJ,
pubmed-author:SongJianpingJ,
pubmed-author:Stricker-KrongradAlainA
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
4130-4
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
|
|
pubmed:year |
2006
|
|
pubmed:articleTitle |
The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.
|
|
pubmed:affiliation |
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. brhuck@hotmail.com
|
|
pubmed:publicationType |
Journal Article
|
