|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
19
|
|
pubmed:dateCreated |
2005-8-22
|
|
pubmed:abstractText |
The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi's greater than 9 and selectivities up to 1000-fold against other serotonin, dopamine and adrenergic receptors. Several compounds were shown to possess weak partial agonist activity in cloned receptors, which translated to antagonism in in vitro studies.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1D,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:AustinNigel ENE,
pubmed-author:AyrtonAndrew DAD,
pubmed-author:ColemanTanyaT,
pubmed-author:CutlerLeanneL,
pubmed-author:GasterLaramie MLM,
pubmed-author:GordonLaurie JLJ,
pubmed-author:HadleyMichael SMS,
pubmed-author:HeightmanTom DTD,
pubmed-author:HollandVicky AVA,
pubmed-author:MiddlemissDerek NDN,
pubmed-author:PardoeSarah LSL,
pubmed-author:PilleuxJean-PierreJP,
pubmed-author:PowlesJeniferJ,
pubmed-author:PriceGary WGW,
pubmed-author:RileyGraham JGJ,
pubmed-author:RobertsClaireC,
pubmed-author:ScottClaire MCM,
pubmed-author:SteanTania OTO,
pubmed-author:TrailBrenda KBK,
pubmed-author:UptonNeilN,
pubmed-author:WatsonJeannette MJM
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
15
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
4370-4
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
pubmed-meshheading:16039851-Administration, Oral,
pubmed-meshheading:16039851-Animals,
pubmed-meshheading:16039851-Biological Availability,
pubmed-meshheading:16039851-Brain Chemistry,
pubmed-meshheading:16039851-Isoquinolines,
pubmed-meshheading:16039851-Ligands,
pubmed-meshheading:16039851-Rats,
pubmed-meshheading:16039851-Receptor, Serotonin, 5-HT1A,
pubmed-meshheading:16039851-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:16039851-Receptor, Serotonin, 5-HT1D,
pubmed-meshheading:16039851-Receptors, Serotonin,
pubmed-meshheading:16039851-Serotonin Antagonists,
pubmed-meshheading:16039851-Serotonin Receptor Agonists,
pubmed-meshheading:16039851-Structure-Activity Relationship
|
|
pubmed:year |
2005
|
|
pubmed:articleTitle |
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.
|
|
pubmed:affiliation |
High Throughput Chemistry, Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow Essex CM19 5AW, UK. Tom.D.Heightman@gsk.com
|
|
pubmed:publicationType |
Journal Article
|
