Linked Life Data

9308022

Source:http://linkedlifedata.com/resource/pubmed/id/9308022

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1997-11-21
pubmed:abstractText
The data presented in this manuscript describe the binding characteristics of the ETA-selective antagonist, [125I]TTA 386 (hexamethylenelmino carbonyl-Leu-Tri-Ala-beta-Ala-Tyr-Phe). This radioligand bound with high affinity and specificity to cloned human ETA receptors and rat mesenteric artery ETA receptors. The apparent dissociation constants (KdS) and maximum binding capacities were 1.0 nM and 8.5 pmol/mg for cloned human ETA receptors and 0.8 nM and 170 fmol/mg for rat mesenteric artery membranes respectively. Binding of [125I]TTA 386 was fast reaching equilibrium by 45 min and 15 min for human ETA and rat mesenteric artery membrane, respectively. Addition of excess unlabeled ligand resulted in the dissociation of bound radioligand from both preparations. Competition of [125I]TTA 386 binding by unlabeled ET-1, ET-3, TTA 386 and BQ123 revealed appropriate ETA pharmacology. This radioligand did not display any binding to cloned human ETB receptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0143-4179
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
345-9
pubmed:dateRevised
2005-11-17
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Binding characteristics of [125I]TTA 386, ETA-selective antagonist.
pubmed:affiliation
Department of Renal Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939, USA.
pubmed:publicationType
Journal Article