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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-12-24
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pubmed:abstractText |
The discovery of a novel series of 5-HT(2C) agonists based on a tricyclic pyrazolopyrimidine scaffold is described. Compounds with good levels of in vitro potency and moderate to good levels of selectivity with respect to the 5-HT(2A) and 5-HT(2B) receptors were identified. One of the analogues (7 g) was found to be efficacious in a sub-chronic weight loss model. A key limitation of the series of compounds was that they were found to be potent inhibitors of the hERG ion channel. Some compounds, bearing polar side chains were identified which showed a much reduced hERG liability however these compounds were sub-optimal in terms of their in vitro potency or selectivity.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aza Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Azepines,
http://linkedlifedata.com/resource/pubmed/chemical/ERG1 potassium channel,
http://linkedlifedata.com/resource/pubmed/chemical/Ether-A-Go-Go Potassium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Heterocyclic Compounds, 3-Ring,
http://linkedlifedata.com/resource/pubmed/chemical/Indenes,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2C,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin 5-HT2 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/pyrimidine
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BrownChristopher JCJ,
pubmed-author:HeifetzAlexanderA,
pubmed-author:MoellerClemensC,
pubmed-author:MuellerStephan GSG,
pubmed-author:NosseBerndB,
pubmed-author:Pedret-DunnAnnaA,
pubmed-author:PrestleJuergenJ,
pubmed-author:PrevostNatachaN,
pubmed-author:ScheuererStefanS,
pubmed-author:SchindlerMarcusM,
pubmed-author:TyeHeatherH,
pubmed-author:WhittakerMarkM
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
34-7
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pubmed:meshHeading |
pubmed-meshheading:21146986-Animals,
pubmed-meshheading:21146986-Aza Compounds,
pubmed-meshheading:21146986-Azepines,
pubmed-meshheading:21146986-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:21146986-Heterocyclic Compounds, 3-Ring,
pubmed-meshheading:21146986-Humans,
pubmed-meshheading:21146986-Indenes,
pubmed-meshheading:21146986-Male,
pubmed-meshheading:21146986-Metabolic Diseases,
pubmed-meshheading:21146986-Pyrimidines,
pubmed-meshheading:21146986-Rats,
pubmed-meshheading:21146986-Rats, Wistar,
pubmed-meshheading:21146986-Receptor, Serotonin, 5-HT2A,
pubmed-meshheading:21146986-Receptor, Serotonin, 5-HT2B,
pubmed-meshheading:21146986-Receptor, Serotonin, 5-HT2C,
pubmed-meshheading:21146986-Serotonin 5-HT2 Receptor Agonists,
pubmed-meshheading:21146986-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders.
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pubmed:affiliation |
Evotec UK Ltd, 114 Milton Park, Abingdon, Oxfordshire OX14 4SA, UK. heather.tye@evotec.com
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pubmed:publicationType |
Journal Article
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