Positron emission tomography with 11C CGP-12177 to assess beta-adrenergic receptor concentration in idiopathic dilated cardiomyopathy.
- 1 April 1993
- journal article
- abstracts
- Published by Wolters Kluwer Health in Circulation
- Vol. 87 (4) , 1169-1178
- https://doi.org/10.1161/01.cir.87.4.1169
Abstract
BACKGROUND Positron emission tomography (PET) with 11C-labeled CGP-12177 (CGP) has been shown to have the potential to noninvasively measure beta-adrenergic receptor concentration in dog heart. The present study was undertaken to evaluate the clinical value of this technique. METHODS AND RESULTS Eight normal subjects and 10 patients with heart failure related to an idiopathic cardiomyopathy were studied. Estimation of beta-receptor concentration was based on a graphic method applied on myocardial PET time-concentration curves obtained after an intravenous injection of 11C-CGP followed 30 minutes later by a coinjection of labeled and unlabeled CGP. The clinical tolerance of these injections was good. Left ventricular concentration of beta-receptors was decreased in patients compared with controls (3.12 +/- 0.51 versus 6.60 +/- 1.18 pmol/mL, respectively; p < 0.001). This 53% decrease agrees with previous in vitro data. In eight of the 10 patients, the beta-receptor concentration obtained from PET was compared with the beta-receptor density determined on left ventricular endomyocardial biopsy samples by in vitro binding technique using 3H-CGP-12177. Results obtained with both techniques were correlated (r = 0.79, p = 0.019). Moreover, decreased beta-receptor concentration correlated with the beta-contractile responsiveness to intracoronary dobutamine infusion (r = 0.83, p = 0.003), indicating a direct link between changes in the receptor number and its biological function. CONCLUSIONS PET appears to be a safe and reliable method of assessing in vivo changes in the number of left ventricular beta-adrenergic receptor sites of patients with idiopathic cardiomyopathy.Keywords
This publication has 17 references indexed in Scilit:
- Asymmetric synthesis of (2S)‐and (2R)‐4‐(3‐t‐butylamino‐2‐hydroxypropoxy)‐benzimidazol‐2‐[11C]‐one ((S)‐and (R)‐[11C]‐CGP 12177) from optically active precursorsJournal of Labelled Compounds and Radiopharmaceuticals, 1991
- Increase of the 40,000-mol wt pertussis toxin substrate (G protein) in the failing human heart.Journal of Clinical Investigation, 1988
- Intracoronary infusion of dobutamine to patients with and without severe congestive heart failure. Dose-response relationships, correlation with circulating catecholamines, and effect of phosphodiesterase inhibition.Journal of Clinical Investigation, 1988
- One hour of myocardial ischemia in conscious dogs increases β-adrenergic receptors, but decreases adenylate cyclase activityJournal of Molecular and Cellular Cardiology, 1988
- Externalization of beta-adrenergic receptors promoted by myocardial ischemiaScience, 1985
- $beta;-Adrenergic function in heart muscle disease and heart failureJournal of Molecular and Cellular Cardiology, 1985
- Plasma Norepinephrine as a Guide to Prognosis in Patients with Chronic Congestive Heart FailureNew England Journal of Medicine, 1984
- [3H]CGP-12177, A β-Adrenergic Ligand Suitable for Measuring Cell Surface ReceptorsJournal of Receptor Research, 1983
- Decreased Catecholamine Sensitivity and β-Adrenergic-Receptor Density in Failing Human HeartsNew England Journal of Medicine, 1982
- Selectivity of Dobutamine for Adrenergic Receptor SubtypesJournal of Clinical Investigation, 1981