|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
7
|
|
pubmed:dateCreated |
2009-7-6
|
|
pubmed:abstractText |
Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepane central constraint that blocks orexin signaling in vivo. In telemetry-implanted rats, oral administration of this antagonist produced a decrease in wakefulness, while increasing REM and non-REM sleep.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jul
|
|
pubmed:issn |
1860-7187
|
|
pubmed:author |
pubmed-author:BednarRodney ARA,
pubmed-author:BoguskyMichael JMJ,
pubmed-author:BrashearKaren MKM,
pubmed-author:BreslinMichael JMJ,
pubmed-author:BrunoJoseph GJG,
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:KoblanKenneth SKS,
pubmed-author:KrausRichard LRL,
pubmed-author:LemaireWeiW,
pubmed-author:LiChunzeC,
pubmed-author:LiYuxingY,
pubmed-author:PrueksaritanontThomayantT,
pubmed-author:ReissDuane RDR,
pubmed-author:RengerJohn JJJ,
pubmed-author:SchreierJohn DJD,
pubmed-author:WhitmanDavid BDB,
pubmed-author:WinrowChristopher JCJ
|
|
pubmed:issnType |
Electronic
|
|
pubmed:volume |
4
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1069-74
|
|
pubmed:meshHeading |
|
|
pubmed:year |
2009
|
|
pubmed:articleTitle |
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, WP14-2, West Point, PA 19486, USA. david_whitman@merck.com
|
|
pubmed:publicationType |
Journal Article
|
