Linked Life Data

21139245

Source:http://linkedlifedata.com/resource/pubmed/id/21139245

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
12
pubmed:dateCreated
2010-12-8
pubmed:abstractText
The 5-HT? receptor (5-HT?R) is a member of the class of recently discovered 5-hydroxytryptamine (5-HT) receptors. Due to the lack of selective 5-HT?R ligands, the cellular signaling mechanisms of the 5-HT?R are poorly understood. We previously developed a cell-based high-throughput screening (HTS) method for the 5-HT?R and screened synthetic chemical compounds. In the present study, we expanded our screening into natural products to find novel 5-HT?R ligands. We found that the ethyl acetate fraction from the root of Caragana sinica (537-18BE) produced the most potent antagonistic activity. After further isolation of 537-18BE, we found that three stilbene derivatives, (+)-?-viniferin, miyabenol C and pallidol, are active constituents of 537-18BE inhibiting the 5-HT?R. Among them, (+)-?-viniferin showed the most potent inhibition, and miyabenol C also produced a considerable inhibition. When examined effects on other neurotransmitters for selectivity, 537-18BE and three stilbene derivatives did not produce any notable effects on 5-HT?, 5-HT?, or muscarinic acetylcholine M1 (M(1)) receptors. Furthermore, 5-HT?R antagonistic effects of (+)-?-viniferin, miyabenol C and pallidol were confirmed on extracellular signal-regulated kinase 1 and 2 (ERK1/2) which exerts effects in downstream pathways of 5-HT?R activation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1347-5215
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
33
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2024-8
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Stilbene derivatives as human 5-HT(6) receptor antagonists from the root of Caragana sinica.
pubmed:affiliation
Korea Institute of Science and Technology, Seoul, Korea.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't