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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2010-7-8
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pubmed:abstractText |
Orexins are excitatory neuropeptides that regulate arousal and sleep. Orexin receptor antagonists promote sleep and offer potential as a new therapy for the treatment of insomnia. In this Letter, we describe the synthesis of constrained diazepanes having a 3,9 diazabicyclo[4.2.1]nonane bicyclic core with good oral bioavailability and sleep-promoting activity in a rat EEG model.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AndersonWayne BWB,
pubmed-author:ColemanPaul JPJ,
pubmed-author:CoxChristopher DCD,
pubmed-author:DoranScott MSM,
pubmed-author:GarsonSusan LSL,
pubmed-author:HarrellC MeachamCM,
pubmed-author:HartmanGeorge DGD,
pubmed-author:McGaugheyGeorgia BGB,
pubmed-author:MercerSwati PSP,
pubmed-author:PrueksaritanontThomayantT,
pubmed-author:ReissDuane RDR,
pubmed-author:RengerJohn JJJ,
pubmed-author:RoeckerAnthony JAJ,
pubmed-author:SchreierJohn DJD,
pubmed-author:TangCuyueC,
pubmed-author:WinrowChristopher JCJ
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pubmed:copyrightInfo |
2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4201-5
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pubmed:meshHeading |
pubmed-meshheading:20610153-Alkanes,
pubmed-meshheading:20610153-Animals,
pubmed-meshheading:20610153-Aza Compounds,
pubmed-meshheading:20610153-Bicyclo Compounds,
pubmed-meshheading:20610153-Biological Availability,
pubmed-meshheading:20610153-Drug Discovery,
pubmed-meshheading:20610153-Electroencephalography,
pubmed-meshheading:20610153-Hypnotics and Sedatives,
pubmed-meshheading:20610153-Rats,
pubmed-meshheading:20610153-Rats, Sprague-Dawley,
pubmed-meshheading:20610153-Receptors, G-Protein-Coupled,
pubmed-meshheading:20610153-Receptors, Neuropeptide
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States. paul_coleman@merck.com
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pubmed:publicationType |
Journal Article
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