PET imaging of myocardial beta-adrenergic receptors with fluorocarazolol: lack of interference by endogenous catecholamines

Journal of Cardiovascular Pharmacology
Cristian SalinasPaul Ernsberger

Abstract

beta-Adrenergic receptor (beta-AR) concentration can be measured in vivo using positron emission tomography (PET) and the high-affinity antagonist [18F]-(S)-fluorocarazolol {[18F]-(S)-FCZ}. However, the influence of endogenous catecholamines on the in vivo binding properties of [18F]-(S)-FCZ should be measured to aid in selection of the model used to estimate receptor concentration based on PET data. Herein we addressed the questions "What is the influence of endogenous catecholamines on the [18F]-(S)-FCZ binding in the heart?" and "In what range are the in vivo concentrations of endogenous beta-AR ligands?" In PET studies, 3 drug regimens were used to manipulate the levels of endogenous catecholamines. The time courses of myocardial concentration of [18F]-(S)-FCZ were compared before and after drug administration. In vitro binding assays and computer simulations were performed to complement the in vivo studies. Despite the large changes of endogenous catecholamines, no significant changes were observed in the [18F]-(S)-FCZ myocardial concentration. In vitro assays showed that (S)-FCZ has an affinity for beta-receptors that is 3900 and 9500 times higher than those of norepinephrine (NE) and epinephrine (EPI), respectively. Comp...Continue Reading

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Citations

Jun 9, 2007·Medical Physics·Cristian SalinasGerald M Saidel
Dec 3, 2017·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Osamu ManabeKeiichiro Yoshinaga

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