Defining the affinity and receptor sub-type selectivity of four classes of endothelin antagonists in clinically relevant human cardiovascular tissues
Abstract
We have compared the endothelin receptor subtype affinity (K(D)) and selectivity of four structural classes of antagonists (peptide, sulphonamide-based, carboxylic acid-based, myceric acid-based) in human cardiovascular tissues to determine whether these are predicted by values reported for human cloned receptors. Additionally, affinities (K(B)) for these antagonists, determined in ET-1-mediated vasoconstriction assays in human blood vessels,...
Paper Details
Title
Defining the affinity and receptor sub-type selectivity of four classes of endothelin antagonists in clinically relevant human cardiovascular tissues
Published Date
Oct 1, 2012
Journal
Volume
91
Issue
13-14
Pages
681 - 686
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