Preclinical evaluation of an 18F-labelled β1-adrenoceptor selective radioligand based on ICI 89406

摘要

PurposeRadioligand binding studies indicate a down-regulation of myocardial β1-adrenoceptors (β1-AR) in cardiac disease which may or may not be associated with a decrease in β2-ARs. We have chosen ICI 89,406, a β1-selective AR antagonist, as the lead structure to develop new β1-AR radioligands for PET and have synthesised a fluoro-ethoxy derivative (F-ICI).