rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2004-9-29
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pubmed:abstractText |
We describe the structure-activity relationships for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as histamine H(4) receptor (H(4)R) antagonists. Furthermore, we identified related benzimidazoles as novel lead compounds for the H(4)R. The ligands have been evaluated by radioligand displacement studies and functional assays for their interaction with both the human histamine H(3) and H(4) receptors and exhibit pK(i) values up to 7.5 at the human H(4)R.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Benzimidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/HRH4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine H1 Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
|
pubmed:issn |
0960-894X
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
14
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
5251-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15454206-Benzimidazoles,
pubmed-meshheading:15454206-Binding, Competitive,
pubmed-meshheading:15454206-Cell Line,
pubmed-meshheading:15454206-Histamine H1 Antagonists,
pubmed-meshheading:15454206-Humans,
pubmed-meshheading:15454206-Indoles,
pubmed-meshheading:15454206-Ligands,
pubmed-meshheading:15454206-Piperazines,
pubmed-meshheading:15454206-Radioligand Assay,
pubmed-meshheading:15454206-Receptors, G-Protein-Coupled,
pubmed-meshheading:15454206-Receptors, Histamine,
pubmed-meshheading:15454206-Structure-Activity Relationship
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pubmed:year |
2004
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pubmed:articleTitle |
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
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pubmed:affiliation |
Istanbul University, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, 34452 Istanbul, Turkey.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|