rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
24
|
pubmed:dateCreated |
2000-12-29
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pubmed:abstractText |
A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indole is a high-affinity (1.2nM), selective (>800 fold over h5-HT2C and hD2 receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
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pubmed:month |
Dec
|
pubmed:issn |
0960-894X
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
18
|
pubmed:volume |
10
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2701-3
|
pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11133072-Administration, Oral,
pubmed-meshheading:11133072-Animals,
pubmed-meshheading:11133072-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:11133072-Binding, Competitive,
pubmed-meshheading:11133072-Biological Availability,
pubmed-meshheading:11133072-Humans,
pubmed-meshheading:11133072-Indoles,
pubmed-meshheading:11133072-Ligands,
pubmed-meshheading:11133072-Piperidines,
pubmed-meshheading:11133072-Rats,
pubmed-meshheading:11133072-Receptors, Dopamine D2,
pubmed-meshheading:11133072-Receptors, Serotonin,
pubmed-meshheading:11133072-Serotonin Antagonists,
pubmed-meshheading:11133072-Structure-Activity Relationship
|
pubmed:year |
2000
|
pubmed:articleTitle |
3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
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pubmed:affiliation |
Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Harlow, Essex, UK. james_crawforth@merck.com
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pubmed:publicationType |
Journal Article
|