Linked Life Data

15714006

Source:http://linkedlifedata.com/resource/pubmed/id/15714006

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2005-4-8
pubmed:abstractText
Endothelin ET(A) receptors on the human astrocytoma 1321N1 cell line were characterized in radioligand binding studies using the ET(A)-selective antagonist radioligand [(3)H]BQ-123. A membrane preparation of the cell line showed a high expression level of ET(A) receptors (B(max) = 128 fmol/mg protein). The K(D) value for [(3)H]BQ-123 (K(D) = 2.29 nmol/l) was comparable to that previously determined at the human neuroblastoma cell line SK-N-MC. The specific labeling of ET(A) receptors on astrocytoma 1321N1 cells by [(3)H]BQ-123 was confirmed by determining the rank order of potency of a series of agonists and antagonists. A competition assay for the screening of potential ET(A) ligands was established and a series of new disubstituted imidazo[1,2-c]pyrimidine and pyrimido[1,6-a]pyrimidine derivatives was investigated. Moderate ET(A) affinity was detected for several derivatives [30-40% inhibition of [(3)H]BQ-123 binding (3 nmol/l) at a concentration of 10 micromol/l]. Astrocytoma 1321N1 cells natively express relatively high levels of ET(A) receptors. They are useful for the screening of potential ET(A) ligands in radioligand binding assays with [(3)H]BQ-123.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0031-7012
pubmed:author
pubmed:copyrightInfo
Copyright (c) 2005 S. Karger AG, Basel
pubmed:issnType
Print
pubmed:volume
74
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
51-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
[H]BQ-123 binding to native endothelin ET(A) receptors in human astrocytoma 1321N1 cells and screening of potential ligands.
pubmed:affiliation
Pharmaceutical Institute, Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Bonn, Germany.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't