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Direct determination of endothelin receptor antagonist levels in plasma using a scintillation proximity assay
- Source :
- Life Sciences. 66:937-945
- Publication Year :
- 2000
- Publisher :
- Elsevier BV, 2000.
-
Abstract
- An assay using scintillation proximity bead technology has been developed suitable for the quantitation of endothelin (ET) receptor antagonists in preclinical and clinical samples of plasma. The assay measures the competitive inhibition of radiolabelled ET-1 binding to ET(A) receptor membranes bound to wheat germ agglutinin (WGA)-coated scintillation proximity assay (SPA) beads in the presence of plasma containing A-127722, a potent orally active, ET(A) selective ET antagonist. The assay requires as little as 50 microl plasma and no extraction procedure is needed. The SPA methodology eliminates the need for the separation of bound from free ligand. Using this method, A-127722 could be directly quantified in rat plasma with a detection limit of 1 ng/ml.
- Subjects :
- Endothelin Receptor Antagonists
Pyrrolidines
CHO Cells
General Biochemistry, Genetics and Molecular Biology
Radioligand Assay
Non-competitive inhibition
Cricetinae
Animals
Humans
General Pharmacology, Toxicology and Pharmaceutics
Chromatography, High Pressure Liquid
Chromatography
Endothelin-1
Receptors, Endothelin
Endothelin receptor antagonist
Chemistry
General Medicine
Ligand (biochemistry)
Endothelin 1
Recombinant Proteins
Wheat germ agglutinin
Rats
Spectrometry, Fluorescence
Scintillation proximity assay
Atrasentan
Scintillation Counting
Endothelin receptor
Subjects
Details
- ISSN :
- 00243205
- Volume :
- 66
- Database :
- OpenAIRE
- Journal :
- Life Sciences
- Accession number :
- edsair.doi.dedup.....03e03870584cfac97e6f9f369baea1ca